Search Result
Results for "
Rat model
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
13
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101481
-
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COX
Apoptosis
MEK
ERK
PPAR
AMPK
NF-κB
Interleukin Related
TNF Receptor
STAT
Wnt
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway .
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- HY-19155A
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ZD-8731
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Angiotensin Receptor
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Cardiovascular Disease
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ICI-D 8731 (compound 5g) is a angiotensin II receptor antagonist with the IC50 of 0.031 μM. ICI-D 8731 shows a rapid and sustained lowering of blood pressure in a renal hypertensive rat model .
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- HY-173142
-
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Drug Derivative
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Neurological Disease
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Neuroprotective agent 7 (Compound 13) is a BBB-penetrable neuroprotective agent. Neuroprotective agent 7 has a powerful neuroprotective effect and can reduce the cerebral infarct area in the MCAO rat model. Neuroprotective agent 7 can be used in the research of diseases such as cerebral ischemia .
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- HY-120710
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-
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- HY-174127
-
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P2Y Receptor
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Neurological Disease
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P2Y1 antagonist 3 (compound 36b) is a blood-brain barrier (BBB)-penetrant P2Y1 antagonist with an IC50 of 0.50 μM. P2Y1 antagonist 3 exhibits protective effects in a rat middle cerebral artery occlusion (MCAO) model and demonstrates neuroprotective activity against oxidative stress by upregulating nuclear Nrf2 protein levels .
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- HY-117132
-
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mGluR
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Neurological Disease
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YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
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-
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- HY-103556
-
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mGluR
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Neurological Disease
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YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
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-
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- HY-101481R
-
|
Reference Standards
COX
Apoptosis
MEK
ERK
PPAR
AMPK
NF-κB
Interleukin Related
TNF Receptor
STAT
Wnt
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Flurbiprofen axetil (Standard) is the analytical standard of Flurbiprofen axetil. This product is intended for research and analytical applications. Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway .
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- HY-176793
-
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JAK
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Infection
Inflammation/Immunology
Cancer
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JAK1-IN-18 (Example 2) is a selective JAK1 inhibitor with an IC50 of 0.15 nM for JAK1 over JAK2 and JAK3. JAK1-IN-18 significantly reduces inflammation in DSS (HY-116282C)-induced ulcerative colitis (UC) mouse models and DNBS(HY-W324435)-induced Crohn's disease (CD) rat models. JAK1-IN-18 can be used for autoimmune diseases (such as inflammatory bowel disease), viral infections (such as HBV infection) and cancers (such as blood cancer) research .
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- HY-176560
-
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Others
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Metabolic Disease
Cancer
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Raloxifene alkene (Compound 101) is a serum cholesterol clearance agent. Raloxifene alkene has significant anti-proliferation activity against breast adenocarcinoma cells. Raloxifene alkene effectively reduces serum cholesterol level without significant uterine weight and increase of number oieosinoohils in the stromallaver of ovarleclomized rat models. Raloxifene alkene can be used for post-menopausasyndrome, particularly osteoporosis, estrogen-dependent breast and uterine carcinoma research .
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- HY-W274652
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IEM-1770
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iGluR
Drug Derivative
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Neurological Disease
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Benzylaspartic acid (IEM-1770), a derivative of aspartic acid, is a NMDA agonist. Benzylaspartic acid has antidepressant activity. Benzylaspartic acid blocks alcohol-abstinence syndrome (AAS) development in chronic alcohol drinking rat models. Benzylaspartic acid can be used for depression research .
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- HY-P991358
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LFA-102; X213
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Estrogen Receptor/ERR
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Cancer
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XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting PRLR/Prolactin Receptor. XOMA-213 inhibits hPRL-dependent growth of BaF3/hPRLR cells (EC50: 0.5 μg/mL). XOMA-213 inhibits PRLR signaling and tumor growth in the Nb2-11-luc xenograft mouse model and the DMBA-induced rat breast cancer model. XOMA-213 can be used in Breast cancer, Hyperprolactinaemia and Prostate cancer research .
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- HY-159931
-
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AAK1
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Neurological Disease
|
HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC50 values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model .
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- HY-W794785
-
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5-HT Receptor
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Neurological Disease
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WAY 208466 is a selective 5-HT6 receptor agonist with an EC50 of 7.3 nM. WAY-208466 increases GABA levels following both acute and chronic administration in the dorsolateral frontal cortex of rat models with stereotaxic surgery. WAY 208466 can be used for anxiety-related disorders like obsessive compulsive disorder (OCD) research .
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- HY-176712
-
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GSNOR
Apoptosis
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Neurological Disease
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GSNOR-IN-1, a prodrug of GSNOR-IN-2 (HY-176275), is a BBB-penetrable S-nitrosoglutathione reductase (GSNOR) inhibitor. GSNOR-IN-1 has significant protective activity against OGD/R-induced injury. GSNOR-IN-1 regulates calcium signaling and synaptic function via Clstn1 S-nitrosation and inhibits neuronal apoptosis. GSNOR-IN-1 significantly reduces infarct volume while improving neurological deficits in ischemic stroke rat models. GSNOR-IN-1 has neuroprotective activity, promising for ischemic stroke research .
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- HY-12706
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-
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- HY-124831
-
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Neurotensin Receptor
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Neurological Disease
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NTRC-844 (compound 8) is a selective antagonist of neurotensin receptor type 2 (NTS2),with the EC50 of 238 nM. NTRC-844 plays an important role in analgesic animal research .
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- HY-17375
-
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Progesterone Receptor
Androgen Receptor
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Endocrinology
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Allylestrenol is an orally active synthetic anti-androgen sexualsteroid. Allylestrenol can prevent miscarriage in vivo. Allylestrenol significantly affects testosterone progesterone level in rat model. Allylestrenol can reduce ventral prostate weight in rat model .
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- HY-P11043
-
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GLP Receptor
Neuropeptide Y Receptor
Arrestin
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Metabolic Disease
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GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
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- HY-111309
-
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Androgen Receptor
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Endocrinology
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LGD-2941 is an orally active, potent and selective androgen receptor modulator. LGD-2941 shows excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. LGD-2941 also improves bone strength in a rat model of post-menopausal osteoporosis .
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- HY-171478
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Drug Derivative
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Others
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SQ 11,447 is a methylurea analogue that demonstrates remarkable resistance to hydrolysis in both in vitro (rat, dog, and human liver homogenates) and in vivo (rat) experimental models.
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- HY-B0712A
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Ro 13-9904 sodium hydRate
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Bacterial
Antibiotic
GSK-3
Aurora Kinase
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Infection
Cancer
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Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
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- HY-B0712AR
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Ro 13-9904 sodium hydRate (Standard)
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Reference Standards
Bacterial
Antibiotic
GSK-3
Aurora Kinase
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Infection
Cancer
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Ceftriaxone (sodium hydrate) (Standard) is the analytical standard of Ceftriaxone (sodium hydrate). This product is intended for research and analytical applications. Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
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- HY-B0712
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Ro 13-9904 free acid
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Bacterial
Antibiotic
GSK-3
Aurora Kinase
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Infection
Inflammation/Immunology
Cancer
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Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
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- HY-B0712S1
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Ro 13-9904-13C2,d3 triethylammonium salt
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Antibiotic
Aurora Kinase
GSK-3
Bacterial
Isotope-Labeled Compounds
|
Infection
Inflammation/Immunology
Cancer
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Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
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- HY-155133
-
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COX
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Inflammation/Immunology
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COX-2-IN-34 (compound 8a) is a selective and orally active inhibitor of COX-2 , with an IC50 of 0.42 μM. COX-2-IN-34 has no gastric ulcer toxicity but has anti-inflammatory effects .
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- HY-B0712R
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Ro 13-9904 free acid (Standard)
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Reference Standards
Bacterial
Antibiotic
GSK-3
Aurora Kinase
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Infection
Inflammation/Immunology
Cancer
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Ceftriaxone (Standard) is the analytical standard of Ceftriaxone. This product is intended for research and analytical applications. Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis[1][2][3][4][5][6][7].
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- HY-17375R
-
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Progesterone Receptor
Reference Standards
Androgen Receptor
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Endocrinology
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Allylestrenol (Standard) is the analytical standard of Allylestrenol. This product is intended for research and analytical applications. Allylestrenol is an orally active synthetic anti-androgen sexualsteroid. Allylestrenol can prevent miscarriage in vivo. Allylestrenol significantly affects testosterone progesterone level in rat model. Allylestrenol can reduce ventral prostate weight in rat model .
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- HY-107527A
-
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GlyT
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Inflammation/Immunology
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Org 25543 is a selective inhibitor of the glycine transporter 2, exhibiting analgesic properties in a rat model of chronic pain.
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- HY-B0712B
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Ro 13-9904
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Antibiotic
GSK-3
Bacterial
Aurora Kinase
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Infection
Inflammation/Immunology
Cancer
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Ceftriaxone sodium salt (Ro 13-9904) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium salt is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium salt is an inhibitor of Aurora B. Ceftriaxone sodium salt has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium salt can be used in the study of bacterial infections and meningitis .
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- HY-170409
-
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Trk Receptor
Apoptosis
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Neurological Disease
Inflammation/Immunology
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BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable .
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- HY-177509
-
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Cholecystokinin Receptor
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Metabolic Disease
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BBL454 (Compound 43) is a Cholecystokinin 2B (CCK2B) receptor agonist. BBL454 induces hyperactivity and improves memory in rat models while it has weak activity on the peripheral CCK2 receptor and no anxiogenic activity. BBL454 increases gastric acid output in anesthetised rat models. BBL454 can be used for diabetes research .
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- HY-168211
-
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Epoxide Hydrolase
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Inflammation/Immunology
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LQ-38 is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 5.2 nM. LQ-38 exhibits anti-inflammatory activity in rat foot edema model and mouse acute pancreatitis model, exhibits analgesic effect in Acetic acid (HY-Y0319)-induced writhing mouse model .
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- HY-N9737
-
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Others
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Neurological Disease
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(−)-Acutumine is a tetracyclic chloroalkaloid that exhibits selective cytotoxicity to cultured human T cells and memory-enhancing properties in the Wistar rat model .
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- HY-119580R
-
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Reference Standards
Others
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Inflammation/Immunology
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Leucocyanidin (Standard) is the analytical standard of Leucocyanidin. This product is intended for research and analytical applications. Leucocyanidin is an active anti-ulcerogenic ingredient was extracted from Litchi Chinensis. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models[1].
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- HY-P1090
-
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Cannabinoid Receptor
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Neurological Disease
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Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
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- HY-P5978
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ANP 127-150 (Rat)
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Natriuretic Peptide Receptor (NPR)
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Cardiovascular Disease
|
Atriopeptin III (ANP 127-150) (rat), a 24-amino acid atrial peptide, is a potent vasodilator and natriuretic/diuretic agent. Atriopeptin III (rat) improves renal functions and decreases blood pressure in a ureter-obstructed rat kidney model. Atriopeptin III (rat) can be used for research of chronic renal failure .
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- HY-W587877
-
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Biochemical Assay Reagents
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Others
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Triundecanoin is a triacylglycerol. Triundecanoin maintain the glucose supplement during fasting through β-oxidation and acetyl-CoA production in rat models .
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- HY-129641
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-
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- HY-B1258
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Aminomethylbenzoic acid; α-Amino-p-toluic acid
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Amino Acid Derivatives
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Cancer
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4-(Aminomethyl)benzoic acid is a competitive inhibitor of PepT1 and has antifibrinolytic activity .
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- HY-15451
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MDA 19
2 Publications Verification
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Cannabinoid Receptor
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Neurological Disease
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MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
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- HY-P1090A
-
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Cannabinoid Receptor
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Neurological Disease
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Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
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- HY-111029
-
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GlyT
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Neurological Disease
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ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model .
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- HY-U00133
-
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Drug Derivative
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Inflammation/Immunology
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HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent. HSR6071 potently inhibits the experimental asthma in rat models .
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- HY-106365
-
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Glucocorticoid Receptor
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Endocrinology
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Rofleponide is a synthetic glucocorticoid that has a high affinity for rat thymic glucocorticoid receptors and has high anti-inflammatory efficacy in experimental animal models .
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- HY-167676
-
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DNA/RNA Synthesis
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Inflammation/Immunology
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Cofpropamine, a caffeine derivative that inhibits polyadenylation, enhances the inhibitory effect of cyclophosphamide (HY-17420) in rat adjuvant arthritis and mouse collagen arthritis models .
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-
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- HY-N3710
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Kumujian G; O-Methylpicrasidine I
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JAK
Apoptosis
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Neurological Disease
Cancer
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Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain .
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- HY-111029A
-
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GlyT
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Others
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ALX-1393 TFA, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model .
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- HY-156696
-
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Na+/H+ Exchanger (NHE)
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Cardiovascular Disease
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S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models .
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- HY-P990302
-
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nAChR
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Neurological Disease
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Anti-Human/Rat/Fish AChR Antibody (Mab35) is an anti-human/rat/fish AChR IgG1 monoclonal antibody. Anti-Human/Rat/Fish AChR Antibody (Mab35) can attack the AChR of neuromuscular junctions. Anti-Human/Rat/Fish AChR Antibody (Mab35) can be used for the construction of myasthenia gravis models .
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- HY-119580
-
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Others
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Inflammation/Immunology
|
Leucocyanidin is an active anti-ulcerogenic ingredient was extracted from Litchi Chinensis. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models .
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- HY-114897
-
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p38 MAPK
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Inflammation/Immunology
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L-167307 is an effective pyrrole-based p38 kinase inhibitor that can reduce secondary paw swelling in rat adjuvant-induced arthritis models .
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- HY-108302
-
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Adrenergic Receptor
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Others
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Nifenalol is a β-adrenergic receptor blocker. Nifenalol inhibits β-adrenoceptor differentiation in right atrium, diaphragm and adipose tissue in a rat model .
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- HY-111755
-
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P2Y Receptor
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Cardiovascular Disease
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Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders .
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- HY-111745
-
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JAK
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Inflammation/Immunology
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Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis .
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- HY-132814
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ATH-1017
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c-Met/HGFR
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Neurological Disease
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Fosgonimeton (ATH-1017) is a hepatocyte growth factor receptor (c-Met/HGFR) agonist. Fosgonimeton has neuroprotective effects in both LPS (HY-D1056) -induced neuroinflammation and Aβ-induced AD models .
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- HY-175668
-
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Potassium Channel
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Neurological Disease
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IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy .
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- HY-171037
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PGBx
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Mitochondrial Metabolism
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Neurological Disease
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Prostaglandin Bx (PGBx) is an oligomer of PGB1 and 15-keto-PGB, which exhibits mitochondrial protective efficacy. Prostaglandin Bx promotes the neurological recovery in rabbits ischemic spinal cord injury model, and maintains the integrity of the gastric mucosa through inhibition of gastric acid secretion in rat gastric ulcer model .
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- HY-128326
-
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MAP3K
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Cardiovascular Disease
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ZAK-IN-1 is an orally active and selective selective leucine-zipper and sterile‑α motif kinase (ZAK) inhibitor with IC50 of 4 nM and KD of 8 nM. ZAK-IN-1 exhibits excellent selectivity against a panel of 403 wild-type kinases. ZAK-IN-1 blocks p38/GATA-4 and JNK/c-Jun signaling and shows promising anti antihypertrophic cardiomyopathy (HCM) efficacy. ZAK-IN-1 can be used for the study of HCM .
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- HY-174986
-
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CGRP Receptor
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Cardiovascular Disease
|
CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki of 0.029 nM. CGRP antagonist 7 Inhibit the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP antagonist 7 can be used for the study of migraine .
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- HY-N2493
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Lawsone
2 Publications Verification
|
Fungal
Apoptosis
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Infection
Cancer
|
Lawsone is an orally active naphthoquinone dye that can be isolated from the leaves of Lawsonia inermis. Lawsone can induce apoptosis. Lawsone has antibacterial, antitumor and antioxidant activities. Lawsone can be used in anti-tumor drug research .
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- HY-169780
-
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TRP Channel
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Neurological Disease
Inflammation/Immunology
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(S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628 (HY-123374). (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin (HY-10448)- and acid-induced Ca 2+-influx with IC50 of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-(HY-153808) induced inflammatory pain models .
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- HY-N2493R
-
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Fungal
Apoptosis
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Infection
Cancer
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Lawsone is an orally active naphthoquinone dye that can be isolated from the leaves of Lawsonia inermis. Lawsone can induce apoptosis. Lawsone has antibacterial, antitumor and antioxidant activities. Lawsone can be used in anti-tumor drug research .
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- HY-111258
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- HY-N14177
-
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Bacterial
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Infection
|
Cyathin A4 has weak activity against Gram-positive bacteria, negative bacteria, actinomycetes and dermatophytes, and has anti-ischemia effect (improving cerebral ischemia in rat model) .
|
-
- HY-N14176
-
|
Bacterial
|
Infection
|
Cyathin A3 has weak activity against Gram-positive bacteria, negative bacteria, actinomycetes and dermatophytes, and has anti-ischemia effect (improving cerebral ischemia in rat model) .
|
-
- HY-P10427
-
|
CXCR
HIV
|
Infection
|
DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models .
|
-
- HY-106856
-
NT-11624
|
iGluR
|
Cancer
|
Dimiracetam is an orally active compound, with anti-neuropathic activity. Dimiracetam inhibits hypersensitivity and neurological alterations, and inhibits Sorafenib (HY-10201)-induced neuropathy in cold stimulation rat models .
|
-
- HY-123179
-
|
Carbonic Anhydrase
|
Cardiovascular Disease
|
Mefruside is an orally active diuretic and has a mild hypotensive effect. Mefruside inhibits the synthesis of urea in an isolated rat liver perfusion model. Mefruside can be used in studies of oedema and hypertension .
|
-
- HY-111219
-
NM-702; NT-702
|
Phosphodiesterase (PDE)
|
Others
|
Parogrelil (hydrochloride) (NM-702) is a phosphodiesterase inhibitor with activity in inhibiting intermittent claudication. Parogrelil (hydrochloride) selectively inhibits PDE3, inhibits human platelet aggregation in vitro and rat aortic contraction, and improves walking distance and plantar surface temperature in the rat femoral artery ligation model, with better effects than cilostazol.
|
-
- HY-172147
-
|
Somatostatin Receptor
|
Neurological Disease
|
SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
|
-
- HY-A0113
-
Ro 31-3113
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
Cilazaprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50=0.7 nM for the rat enzyme) and an active metabolite of Cilazapril (HY-A0043). It decreases creatine kinase release in primary neonatal rat cardiac myocytes in an in vitro model of ischemia-reperfusion injury induced by hypoxia and reoxygenation when used at a concentration of 10 μM.3 Intra-arterial administration of cilazaprilat (3 μg/kg per minute) increases coronary blood flow and fractional shortening in a dog model of coronary hypoperfusion-induced myocardial ischemia.
|
-
- HY-P990107
-
|
TGF-β Receptor
|
Cancer
|
Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
|
-
- HY-156259
-
|
Acyltransferase
|
Metabolic Disease
|
PF-07202954 is a weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2. PF-07202954 lowers liver triglyceride content in a Western-diet-fed rat model .
|
-
- HY-119580B
-
2,3-trans-3,4-trans-Leucocyanidin; 3,4-trans-Leucocyanidin; (2R,3S,4R)-Leucocyanidin
|
Drug Isomer
|
Inflammation/Immunology
|
(+)-Leucocyanidin is the isoform of Leucocyanidin (HY-119580), is an active anti-ulcerogenic ingredient was extracted from Litchi Chinensis. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models .
|
-
- HY-164040
-
|
Somatostatin Receptor
|
Metabolic Disease
|
Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model .
|
-
- HY-161705
-
|
Apoptosis
|
Neurological Disease
|
Anti-apoptotic agent 1 (Compound B4) exhibits neuroprotective activity and good pharmacokinetic properties. Anti-apoptotic agent 1 inhibits apoptosis, prevents stroke recurrence in photothrombotic rat model .
|
-
- HY-121810
-
|
Dopamine Transporter
|
Others
|
LBT-999 is a phenyltropane derivative used for positron emission tomography (PET) exploration of the dopamine transporter (DAT). It has high affinity binding to DAT on rat striatal membranes and human postmortem brain slices in vitro, high uptake in the striatum in rat and baboon models in vivo, and its binding can be blocked by specific compounds.
|
-
- HY-15451R
-
|
Reference Standards
Cannabinoid Receptor
|
Neurological Disease
|
MDA 19 (Standard) is the analytical standard of MDA 19. This product is intended for research and analytical applications. MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
|
-
- HY-116638
-
|
Lipoxygenase
|
Endocrinology
|
AHR-5333 is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity .
|
-
- HY-142123
-
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
Fluocortolone is an orally active anti-inflammatory agent that effectively reduces plasma fibrinogen levels. Fluocortolone inhibits Mycobacterium butyricum-induced foot edema in a rat model of adjuvanted joint inflammation (3-12 mg/kg) .
|
-
- HY-129103
-
|
Dopamine Receptor
|
Neurological Disease
|
A-412997 is a selective Dopamine D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors. A-412997 improves short term memory and cognitive properties in rodent models .
|
-
- HY-131545
-
NT-702 free base; NT-702 free base
|
Phosphodiesterase (PDE)
|
Others
|
Parogrelil (NT-702 free base) is a compound with intermittent claudication inhibitory activity that inhibits PDE3, inhibits platelet aggregation and vasoconstriction, and improves walking distance and plantar surface temperature in a rat experimental model.
|
-
- HY-W987949
-
|
Others
|
Neurological Disease
|
Z-4105 (formula l) is a nootropic agent. Z-4105 restores the amnesic effect of electroconvulsive ehock (ECS) and methylazoxymethanol acetate (MAM), improving learning and memory function. Z-4105 increases the activity of the brain cholinergic system without affecting other neurotransmitter systems. Z-4105 significantly attenuates the neuropathic pain induced by chronic constrictive lesion (CCl) in the sciatic nerve of rat hind leg models and in the ligament of rat spinal nerve models. Z-4105 can be used for neuropathic pain and cerebral dysfunctional disorders research .
|
-
- HY-119279
-
|
Histamine Receptor
|
Inflammation/Immunology
|
VUF 10214 is a H4 receptor ligand with a pKi of 8.25. VUF 10214 exhibits significant anti-inflammatory activity in a carrageenan-induced paw edema rat model and can be used for research in the field of inflammatory diseases .
|
-
- HY-173083
-
|
Cannabinoid Receptor
|
Neurological Disease
|
MDA7 is the selective agonist for cannabinoid receptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models .
|
-
- HY-163756
-
-
- HY-158056
-
|
GLUT
URAT1
|
Metabolic Disease
|
URAT1/GLUT9-IN-1 (compound 29) can inhibit both uric acid transporter 1 (URAT1) (IC50=2.01 μM) and glucose transporter 9 (GLUT9) (IC50=18.21 μM). URAT1/GLUT9-IN-1 exhibits favorable pharmacokinetic properties and oral bioavailability. URAT1/GLUT9-IN-1 can be uesd for gout and hyperuricemia research .
|
-
- HY-147719
-
|
COX
|
Inflammation/Immunology
|
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity .
|
-
- HY-163148
-
-
- HY-12694
-
R-108512
|
5-HT Receptor
Apoptosis
Autophagy
|
Metabolic Disease
Cancer
|
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-12694R
-
|
5-HT Receptor
Apoptosis
Autophagy
|
Metabolic Disease
Cancer
|
Prucalopride (succinate) (Standard) is the analytical standard of Prucalopride (succinate). This product is intended for research and analytical applications. Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-B0647A
-
-
- HY-163368
-
|
HDAC
|
Inflammation/Immunology
|
HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat .
|
-
- HY-116208
-
KU-1257
|
Histamine Receptor
|
Inflammation/Immunology
|
Dalcotidine (KU-1257) is an orally active and competitive histamine H2 receptor antagonist. Dalcotidine promotes the healing of chronic ulcers and inhibits gastric acid secretion .
|
-
- HY-148258
-
-
- HY-101666
-
|
Deubiquitinase
Apoptosis
MDM-2/p53
|
Metabolic Disease
Cancer
|
HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research .
|
-
- HY-116638A
-
|
Lipoxygenase
|
Endocrinology
|
AHR-5333 mandelate is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 mandelate exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity .
|
-
- HY-121191
-
N1,N8-Bisnorcymserine; (-)-Bisnorcymserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate .
|
-
- HY-W754020
-
|
Histamine Receptor
|
Others
|
Elbanizine inhibits histamine, bradykinin, histamin-release from rat mast cells (IC50 of 0.26 μM) and the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction. Elbanizine exhibits antiallergic and antiasthmatic in guinea pig model .
|
-
- HY-P1010
-
Z-LEHD-FMK
Maximum Cited Publications
13 Publications Verification
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-120481
-
|
FAAH
|
Neurological Disease
|
JNJ-40413269 is an inhibitor for FAAH, that inhibits human FAAH and rats FAAH with IC50 of 28 nM and 270 nM. JNJ-40413269 exhibits analgesic efficacy in rat spinal nerve ligation model and exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-B0954A
-
|
mAChR
|
Endocrinology
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
|
-
- HY-13762
-
|
Cytochrome P450
|
Cancer
|
Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-13762A
-
|
Cytochrome P450
|
Cancer
|
Tesmilifene hydrochloride is an antihistamine agent and a chemical sensitizer. Tesmilifene hydrochloride targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene hydrochloride overcomes multidrug resistance .
|
-
- HY-B2141
-
|
NO Synthase
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Others
Metabolic Disease
|
Bendazol is an orally effective antihypertensive agent. Bendazol acts directly on vascular smooth muscle to dilate blood vessels and reduce peripheral resistance, thereby improving blood circulation. Bendazol significantly inhibits the development of myopia in rabbit models. Bendazol can regulate kidney function by increasing the activity of NO synthase in the rat model of nephrogenic hypertension. In addition, Bendazol has an effect on sexual behavior and spermatogenesis in male rats .
|
-
- HY-14886
-
MEN16132 free base
|
Bradykinin Receptor
|
Cardiovascular Disease
Neurological Disease
|
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model .
|
-
- HY-19590
-
Ro 15-1570
|
Drug Derivative
|
Cancer
|
Etarotene (Ro 15-1570) is a derivative of Arotinoid (HY-106735). Etarotene is an orally active antitumor agent against DMBA (HY-W011845)-induced mammary tumor and causes toxic symptoms of hypervitaminosis A in rat model .
|
-
- HY-129736A
-
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
P32/98 a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model .
|
-
- HY-B1619R
-
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Cromolyn (Standard) is the analytical standard of Cromolyn. This product is intended for research and analytical applications. Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
|
-
- HY-B0320A
-
Cromoglycate disodium; Cromoglicic acid disodium; FPL-670
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Cromolyn (Cromoglycate) disodium is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn disodium is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn disodium can be used in the research of bronchial asthma. In addition, Cromolyn disodium has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
|
-
- HY-B1619
-
Cromoglycate; Cromoglicic acid; FPL-670 free acid
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
|
-
- HY-170918
-
|
Potassium Channel
|
Others
|
BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC50 of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model .
|
-
- HY-19225
-
KA-672 hydrochloride; Anseculin hydrochloride
|
iGluR
|
Neurological Disease
|
Ensaculin is an NMDA receptor channel blocker. Ensaculin has neuroprotective effects in NMDA toxicity models and promotes neuronal growth in primary cultures of rat brain cells. Ensaculin has the potential to be developed as an anti-dementia drug that acts on various neurotransmitter systems .
|
-
- HY-110180
-
|
mGluR
|
Neurological Disease
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
|
-
- HY-P1010A
-
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-18734
-
-
- HY-14364
-
|
Histamine Receptor
|
Inflammation/Immunology
|
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model .
|
-
- HY-127165
-
HP 029 free base; Hydroxytacrine
|
Cholinesterase (ChE)
|
Neurological Disease
|
Velnacrine (HP 029 free base) is an inhibitor for acetylcholinesterase (AChE), with an IC50 of 3.27 μM. Velnacrine reverses the Scopolamine (HY-N0296)-induced amnesia in rat models, and exhibits acute toxicity with LD50 of 65 mg/kg .
|
-
- HY-18734A
-
-
- HY-162650
-
|
ClpP
|
Cancer
|
SL44 is an agonist for human caseinolytic protease P (HsClpP), with an EC50 of 1.30 μM. SL44 inhibits the proliferation of LM3 with an IC50 of 3.1 μM. SL44 induces apoptosis in HCC cells, through the degradation of respiratory chain complex subunits. SL44 exhibits antitumor efficacy in mouse models without obvious toxicity (LD50=400 mg/kg). SL44 exhibits good pharmacokinetic characters in rat models .
|
-
- HY-170499
-
BI02982816
|
mGluR
|
Neurological Disease
|
VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
|
-
- HY-P3199
-
|
PKC
|
Inflammation/Immunology
|
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction .
|
-
- HY-129736
-
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
P32/98 hemifumarateis a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 hemifumarate improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model .
|
-
- HY-159090
-
|
Calcium Channel
Angiotensin Receptor
|
Cardiovascular Disease
|
AT1R antagonist 3 (Compound 1) is an antagonist for angiotensin II type 1 receptor (AT1R) and an inhibitor for calcium channel type-L CaV1.2 (IC50=0.57 μM). AT1R antagonist 3 exhibits vasodilation efficacy in solated rat aorta (10 μM, 88.7%) and antihypertensive efficacy in rat models .
|
-
- HY-B1279A
-
Dipyrone; Methamizole sodium
|
COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
Metamizole sodium (Dipyrone) is an orally active cyclooxygenase (COX) inhibitor. Metamizole sodium can inhibit cell proliferation and promote cell apoptosis. Metamizole sodium has anti-inflammatory and antioxidant activities. Metamizole sodium is an antipyretic, analgesic and spasmolytic agent. .Metamizole sodium can be used in research to relieve a variety of pain .
|
-
- HY-B1279
-
Dipyrone hydRate; Methamizole sodium hydRate
|
COX
Apoptosis
|
Inflammation/Immunology
|
Metamizole sodium hydrate (Dipyrone) is an orally active cyclooxygenase (COX) inhibitor.. Metamizole sodium hydrate can inhibit cell proliferation and promote cell apoptosis. Metamizole sodium hydrate has anti-inflammatory and antioxidant activities. Metamizole sodium hydrate is an antipyretic, analgesic and spasmolytic agent. Metamizole sodium hydrate can be used in research to relieve a variety of pain .
|
-
- HY-B1279R
-
Dipyrone hydRate (Standard); Methamizole sodium hydRate (Standard)
|
Reference Standards
COX
Apoptosis
|
Inflammation/Immunology
|
Metamizole (sodium hydrate) (Standard) is the analytical standard of Metamizole (sodium hydrate). This product is intended for research and analytical applications. Metamizole sodium hydrate (Dipyrone) is an orally active cyclooxygenase (COX) inhibitor.. Metamizole sodium hydrate can inhibit cell proliferation and promote cell apoptosis. Metamizole sodium hydrate has anti-inflammatory and antioxidant activities. Metamizole sodium hydrate is an antipyretic, analgesic and spasmolytic agent. Metamizole sodium hydrate can be used in research to relieve a variety of pain .
|
-
- HY-138063
-
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
Siegeskaurolic acid is an orally active anti-inflammatory agent. Siegeskaurolic acid inhibits the productions of nitric oxide (NO), prostaglandin E(2) (PGE(2)), tumor necrosis factor-alpha (TNF-alpha) and the activationon of nuclear factor-kappaB .
|
-
- HY-13224
-
|
Kinesin
Apoptosis
Mitosis
|
Cancer
|
AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity .
|
-
- HY-162511
-
|
Dopamine Transporter
Serotonin Transporter
|
Others
|
IP2015 is an inhibitor for monoamine reuptake, that inhibits the reuptake of dopamine, serotonin (5-HT), and noradrenaline. IP2015 increases release of central dopamine and peripheral nitric oxide (NO), causes the NO-mediated relaxation of erectile tissue, and thus induces erection in rat model .
|
-
- HY-P3498
-
ZP1846
|
GCGR
|
Others
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model .
|
-
- HY-P1694
-
|
Bradykinin Receptor
|
Cardiovascular Disease
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-Y0816
-
|
Biochemical Assay Reagents
|
Others
|
(S)-Mandelic Acid is a (S)-enantiomer of Mandelic Acid (HY-W015591). (S)-Mandelic Acid undergoes one-directional chiral inversion to (R)-Mandelic Acid in rat models. (S)-Mandelic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
|
-
- HY-10427
-
NRI-022
|
Histone Methyltransferase
|
Neurological Disease
|
WAY-260022 is a selective norepinephrine reuptake inhibitor with potent inhibitory activity on norepinephrine reuptake. WAY-260022 exhibits excellent selectivity in inhibiting serotonin and dopamine transporters. WAY-260022 also showed oral efficacy in a rat model of thermoregulatory dysfunction .
|
-
- HY-163702
-
|
Adrenergic Receptor
mAChR
|
Inflammation/Immunology
|
CHF-6550 is an antagonist for muscarinic M3 receptor and an agonist for β2 adrenoceptor (MABA), with pKi of 9.3 and 10.6, respectively. CHF-6550 exhibits good hepatocyte clearance in rat models and good pharmacokinetic characteristics in guinea pigs .
|
-
- HY-161896
-
|
GABA Receptor
|
Neurological Disease
|
Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED50 =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models .
|
-
- HY-159928
-
-
- HY-164605
-
|
Aldehyde Dehydrogenase (ALDH)
|
Metabolic Disease
|
(6S)-CP-470711 (Compound 8) is an inhibitor for sorbitol dehydrogenase, that inhibits human and rat SDH with IC50 of 19 nM and 27 nM. (6S)-CP-470711 ameliorates the Streptozotocin (HY-13753)-induced diabetes in rats models .
|
-
- HY-131416
-
|
Others
|
Inflammation/Immunology
|
DD-3305 is an anti-inflammatory agent with comparable anti-inflammatory activity to the known anti-inflammatory agent indomethacin (HY-14397). In a carrageenin-induced rat inflammation model, DD-3305 was effective in inhibiting chronic and acute inflammation as well as induced allergies. .
|
-
- HY-119035
-
|
Platelet-activating Factor Receptor (PAFR)
|
Inflammation/Immunology
|
R-75317 is a specific platelet-activating factor (PAF) antagonist. R-75317 can prevent the decline in creatinine clearance (Ccr) in a rat model of glomerulonephritis induced by the injection of antibodies extracted from rabbits against rat glomerular basement membrane (GBM) antigens, delay the onset of proteinuria, and improve glomerular hypertrophy, mesangial matrix proliferation, and interstitial fibrosis. R-75317 may be useful in the study of glomerulonephritis .
|
-
- HY-107969
-
|
Dopamine Receptor
COX
NO Synthase
|
Neurological Disease
Cancer
|
Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model .
|
-
- HY-107510
-
|
mGluR
|
Neurological Disease
|
YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models .
|
-
- HY-147214
-
|
YAP
|
Cancer
|
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
|
-
- HY-P10580
-
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-177506
-
|
Cholecystokinin Receptor
|
Metabolic Disease
|
FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research .
|
-
- HY-A0119
-
Sodium nitroprusside dihydRate; Sodium Nitroferricyanide(III) DihydRate
|
Autophagy
|
Cardiovascular Disease
Cancer
|
Nitroprusside disodium dehydrate (Sodium nitroprusside dihydrate) is a vasodilator that available for the research of acute hypertension, heart failure. Nitroprusside disodium dehydrate induces autophagy in glutathione-depleted osteoblasts. Nitroprusside disodium dehydrate acts as a nitric oxide (NO) donor in a rat intestinal ischemia reperfusion model .
|
-
- HY-110157
-
|
Estrogen Receptor/ERR
|
Neurological Disease
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .
|
-
- HY-124378
-
|
MAGL
|
Inflammation/Immunology
|
MAGL-IN-17 (Compound ) is an inhibitor for MAGL with a Ki of 0.4 μM. MAGL-IN-17 inhibits mouse MAGL and rat MAGL with IC50 of 0.18 and 0.24 μM. MAGL-IN-17 exhibits anti-inflammatory activity in mouse experimental autoimmune encephalitis models .
|
-
- HY-173117
-
|
CaMK
|
Cardiovascular Disease
Cancer
|
RA306 is an orally active CAMK2 inhibitor. RA306 can block the PEAK1/CAMK2 signaling pathway. RA306 inhibits the proliferation, migration, and invasion of breast cancer cells and has anti-tumor activity. In addition, RA306 can improve dilated cardiomyopathy in mice and can be used in the research of heart diseases .
|
-
- HY-137978A
-
GNS561 hydrochloride
|
Palmitoyl Protein Thioesterase (PPT)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Ezurpimtrostat hydrochloride (compound 2-3) is a potent and orally active anti-fibrotic agent. Ezurpimtrostat hydrochloride reduces significantly the liver fibrosis in DEN (diethyl nitrosamine) cirrhotic rat model. Ezurpimtrostat hydrochloride can be used for the research of fibrosis, cancer, autophagy and cathepsins B (CTSB), L (CTSL) and D (CTSD) related diseases .
|
-
- HY-P1091
-
|
Cannabinoid Receptor
|
Neurological Disease
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-125928
-
|
Sodium Channel
|
Neurological Disease
|
AA43279 is an in gamma-aminobutyric acid (GABA) fast-firing interneurons located activator for Nav1.1 channel (SCN1A) with an EC50 of 9.5 μM. AA43279 enhances specific neuronal firing activity in vitro, and exhibits anticonvulsant activity in rat MEST model .
|
-
- HY-113906
-
|
GHSR
|
Metabolic Disease
|
GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models .
|
-
- HY-156613
-
EP-7041
|
Factor XI
|
Infection
|
Frunexian (EP-7041) is a selective and potent inhibitor of coagulation factor XI/activated factor XI, targeting to factor XIa. Frunexian exhibits antithrombotic activity, with no bleeding liability in rat mesenteric arterial puncture model. Frunexian can be used in extracorporeal membrane oxygenation (ECMO) research .
|
-
- HY-163646
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
(Rac)-TZ3O is the (Rac) isomer of TZ3O. TZ3O is an anticholinergic compound with neuroprotective activity. TZ3O improves memory impairment and cognitive decline in a scopolamine-induced Alzheimer's disease rat model and can be used in the study of Alzheimer's disease.
|
-
- HY-N8458
-
NSC 272693
|
PGE synthase
|
Inflammation/Immunology
|
Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity. It inhibits prostaglandin synthetase (IC50=424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.
|
-
- HY-142123R
-
|
Glucocorticoid Receptor
Reference Standards
|
Inflammation/Immunology
|
Fluocortolone (Standard) is the analytical standard of Fluocortolone. This product is intended for research and analytical applications. Fluocortolone is an orally active anti-inflammatory agent that effectively reduces plasma fibrinogen levels. Fluocortolone inhibits Mycobacterium butyricum-induced foot edema in a rat model of adjuvanted joint inflammation (3-12 mg/kg) .
|
-
- HY-113322
-
3-Hydroxyquinidine
|
Drug Metabolite
|
Cardiovascular Disease
|
3-Hydroxyquinine is a metabolite of Quinidine (HY-B1751). 3-Hydroxyquinine prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in an isolated rat heart reperfusion arrhythmia model in a concentration-dependent manner. 3-Hydroxyquinine can be used in the study of cardiac arrhythmias .
|
-
- HY-128976
-
DHED
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor proagent of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain .
|
-
- HY-13533
-
NSC 682691; 4-Demethylpenclomedine
|
Drug Metabolite
|
Cancer
|
DMPEN (NSC 682691) (4-Demethylpenclomedine) is an alkylating metabolite of Penclomedine (HY-106401). DMPEN has an antitumor activity. DMPEN does not induce Purkinje cells loss with no significant neurocerebellar toxicity in rat cerebellum models. DMPEN can be used for cancers like breast and brain cancer research .
|
-
- HY-P10580A
-
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-12378
-
BQ-123
2 Publications Verification
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-101096
-
MK-8998; CX-8998; JZP385
|
Calcium Channel
|
Neurological Disease
Cancer
|
Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-123904
-
|
iGluR
|
Neurological Disease
|
UoS12258 is a selective positive allosteric modulator of AMPA receptor. UoS12258 enhances AMPA receptor‐mediated synaptic transmission. UoS12258 improves performance in cognition rat models, including Scopolamine (HY-N0296)‐impaired rats and water maze learning and retention in aged rats .
|
-
- HY-P10898
-
-
- HY-162584
-
|
TRP Channel
|
Others
|
TRPC5-IN-6 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC5-IN-6 has good biosafety and low liver and kidney toxicity, and is expected to play an important role in the treatment of chronic kidney disease (CKD) .
|
-
- HY-B0885
-
(±)-Econazol
|
Fungal
Bacterial
Calcium Channel
Cytochrome P450
|
Infection
Metabolic Disease
|
Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage .
|
-
- HY-157936
-
|
iGluR
|
Neurological Disease
|
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke .
|
-
- HY-14305
-
|
p38 MAPK
|
Inflammation/Immunology
|
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis .
|
-
- HY-P990117
-
|
Integrin
|
Cardiovascular Disease
Cancer
|
Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
|
-
- HY-155737
-
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-155739
-
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-155738
-
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-164320
-
|
Others
|
Cancer
|
Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-107526
-
(Rac)-NFPS
|
GlyT
|
Neurological Disease
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively . NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion .
|
-
- HY-119152
-
|
Insulin Receptor
Tyrosinase
Akt
|
Others
|
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model .
|
-
- HY-119378
-
CX 295
|
Proteasome
Apoptosis
|
Neurological Disease
|
AK 295 (CX 295) is a calpain inhibitor that inhibits apoptosis through a calpain-dependent pathway. AK 295 improves neurological function in a rat model of spinal cord injury (SCI). AK 295 can be used in the study of neurodegenerative diseases, such as bulbar amyotrophy, stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis .
|
-
- HY-18759
-
|
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model .
|
-
- HY-13762S
-
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cancer
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-P1091A
-
|
Cannabinoid Receptor
|
Neurological Disease
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-161506
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
PDE1-IN-7 (Compound 13h) is a selective inhibitor of bPDE1 (IC50= 10 nM). PDE1-IN-7 exhibits significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model. PDE1-IN-7 can be used for research in liver fibrosis .
|
-
- HY-110199
-
|
TRP Channel
|
Neurological Disease
|
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models .
|
-
- HY-12378A
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-103327
-
|
Cannabinoid Receptor
|
Metabolic Disease
|
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-157796
-
|
Adrenergic Receptor
|
Metabolic Disease
|
β2AR agonist 4 (compound A19) is a potent and selective β2-Adrenoceptor agonist with an EC50 of 3.7 pM. β2AR agonist 4 suppresses the inflammatory cytokines and leukocytes upregulation and improves lung function in COPD rat model .
|
-
- HY-W742532
-
N-Ethyl-nor-LSD
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
ETH-LAD (N-Ethyl-nor-LSD) is an activator for 5-HT2A receptor with Ki of 5.1 nM. ETH-LAD exhibits affinity for dopamine receptor D1 and dopamine receptor D2 with Ki of 22.1 nM and 4.4 nM. ETH-LAD acts as psychoactive substance in rat model .
|
-
- HY-P10977
-
|
Sodium Channel
RIP kinase
|
Neurological Disease
|
Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease .
|
-
- HY-W783623
-
DG(22:6/0:0/22:6); 1,3-Didocosahexaenoin
|
Biochemical Assay Reagents
|
Cardiovascular Disease
|
1,3-Didocosahexaenoyl glycerol (DG(22:6/0:0/22:6); 1,3-Didocosahexaenoin) is an ω-3 polyunsaturated fatty acid, which exhibits cardioprotective effects in rat myocardial ischemia/reperfusion (I/R) injury model through conjugation with Poly-l-glutamic acid (PGA) .
|
-
- HY-N8249
-
|
nAChR
Interleukin Related
|
Inflammation/Immunology
|
Cynandione A is an acetophenone that can be isolated from Cynanchum Wilfordii Radix. Cynandione A protects hepatocytes and cortical neurons from toxicity and improves neurological deficits in a rat model of cerebral ischemia. On the other hand, cynandione A has significant anti-inflammatory effects and inhibits inflammation by activating macrophage α7 nAChR and IL-10 expression .
|
-
- HY-155126
-
|
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
LZWL02003 is an anti-neuroinflammatory agent. LZWL02003 has protective effect on MPP +-induced neuronal damage, and reduces the expression of ROS. LZWL02003 improves cognition, memory, learning, and athletic ability in a Rotenone (HY-B1756)-induced PD rat model. LZWL02003 can be used for research of neurodegenerative disease .
|
-
- HY-122051
-
AC1903
1 Publications Verification
|
TRP Channel
|
Metabolic Disease
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .
|
-
- HY-174311
-
|
Glycosidase
|
Neurological Disease
|
GT-02216 can bind to GCase allosterically and enhance its activity. GT-02216 enhances the activity of GCase in primary human fibroblasts. GT-02216 reduces the Tau accumulation in mutant GBA1 fibroblasts. GT-02216 protects the hippocampal primary neurons challenged with Tau oligomer in rat model .
|
-
- HY-164532
-
|
Chloride Channel
|
Metabolic Disease
|
NS3736 is an orally effective chloride channel inhibitor that can be used for the research of osteoporosis. NS3736 targets the CIC-7 channel in osteocytes, blocks osteoclast acidification and resorption in vitro, with IC50=30 μM. In a rat model of ovariectomy-induced osteoporosis, NS3736 can enhance bone strength and bone density .
|
-
- HY-105351
-
|
Neprilysin
|
Cardiovascular Disease
|
CGS25155 is an orally active neutral endopeptidase 24.11 (NEP 24.11) inhibitor with an IC50 of 3 nM. CGS25155 can slow down the degradation of the cardiac hormone atrial natriuretic peptide (ANP) and exhibits antihypertensive activity in the DOCA-salt induced rat hypertension model. CGS25155 can be used in cardiovascular disease research .
|
-
- HY-P11245
-
|
Amylin Receptor
|
Metabolic Disease
|
NN1213 (Peptide 21), a long-acting human amylin peptide analog, is a selective Amylin receptor agonist with an EC50 of 0.177 and 0.262 nM for hAMY3R and rAMY3R, respectively. NN1213 significantly reduces appetite in rat and dog models. NN1213 can be used for antiobesity research .
|
-
- HY-168084
-
|
Interleukin Related
|
Inflammation/Immunology
|
IL-17-IN-1 (26) is an orally active IL-17 inhibitor, with IC50 values of 0.013 μM and 0.004 μM for IL-17A and IL-6 release, respectively. IL-17-IN-1 (26) effectively reduces knee swelling in a rat arthritis model .
|
-
- HY-117839
-
|
Cholecystokinin Receptor
|
Neurological Disease
|
PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
|
-
- HY-P11245A
-
|
Amylin Receptor
|
Metabolic Disease
|
NN1213 acetate (Peptide 21), a long-acting human amylin peptide analog, is a selective Amylin receptor agonist with an EC50 of 0.177 and 0.262 nM for hAMY3R and rAMY3R, respectively. NN1213 acetate significantly reduces appetite in rat and dog models. NN1213 acetate can be used for antiobesity research .
|
-
- HY-169963
-
|
Phosphodiesterase (PDE)
|
Others
|
PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model .
|
-
- HY-101418
-
|
P2X Receptor
|
Neurological Disease
|
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
|
-
- HY-W587784
-
|
PPAR
|
Metabolic Disease
|
Norbixin is a carotenoid that has been found in B. orellana.It binds to PPARγ in a cell-free assay (Ki = 1.15 μM) . Norbixin attenuates hyperglycemia, hyperinsulinemia, and insulin resistance, as well as decreases serum lipid levels and cardiac levels of thiobarbituric acid reactive substances (TBARS) and glutathione (GSH) in a rat model of cardio-metabolic syndrome .
|
-
- HY-N0265
-
-
- HY-135115
-
3,4-DHPEA-EA
|
α-synuclein
HDAC
Adrenergic Receptor
|
Inflammation/Immunology
|
Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histone deacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasma leptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
|
-
- HY-W110138
-
|
DNA/RNA Synthesis
Cytochrome P450
ROCK
|
Cancer
|
Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
|
-
- HY-107969R
-
|
Dopamine Receptor
Reference Standards
COX
NO Synthase
|
Neurological Disease
|
Haloperidol decanoate (Standard) is the analytical standard of Haloperidol decanoate. This product is intended for research and analytical applications. Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model .
|
-
- HY-18734AR
-
|
NO Synthase
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
Carboxy-PTIO (potassium) (Standard) is the analytical standard of Carboxy-PTIO (potassium). This product is intended for research and analytical applications. Carboxy-PTIO potassium is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO potassium can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model .
|
-
- HY-113427
-
|
Endogenous Metabolite
Bcl-2 Family
Apoptosis
|
Cardiovascular Disease
Cancer
|
trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
|
-
- HY-126835
-
|
Amino Acid Derivatives
|
Cancer
|
A 924 is an amino acid derivative-based, orally active antitumor agent. A 924 is effective in inhibiting ascites tumors in rat models by intraperitoneal injection or oral administration. The LD50 of A 924 in mice is >1.5 g/kg and >4.5 g/kg by intraperitoneal injection or oral administration, respectively. A 924 does not cause teratogenicity or adverse reactions in normal or pregnant mice .
|
-
- HY-110099
-
|
CXCR
|
Inflammation/Immunology
|
(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model .
|
-
- HY-122063
-
|
NO Synthase
|
Inflammation/Immunology
|
FR260330 is a selective, orally active inhibitor for inducible nitric oxide synthase (iNOS) through suppression of iNOS dimerization. FR260330 inhibits the NO accumulation in rat splenocytes and human DLD-110 cells, with IC50 of 27 and 10 nM. FR260330 ameliorates the Lipopolysaccharides (HY-D1056)-induced inflammatory diseases in rats model .
|
-
- HY-155819
-
|
mAChR
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .
|
-
- HY-153091
-
|
Adrenergic Receptor
5-HT Receptor
Sigma Receptor
|
Neurological Disease
|
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .
|
-
- HY-114753
-
CR-2249; XY-2401
|
iGluR
|
Neurological Disease
|
Neboglamine (CR-2249; XY-2401) is a modulator for N-methyl-D-aspartate (NMDA) receptor. Neboglamine increases the levels of fos-like immunoreactivity (FLI)-positive cells in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus in rat models, .restores NMDA (HY-17551) -mediated neurotransmitter release, and inhibits phencyclidine-induced hyperlocomotion .
|
-
- HY-134521
-
|
COX
|
Inflammation/Immunology
|
Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
|
-
- HY-112460
-
|
CDK
|
Cancer
|
CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an IC50 of 60 nM .
|
-
- HY-158688
-
|
PI3K
|
Inflammation/Immunology
|
PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC50 of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of T cells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .
|
-
- HY-172419
-
GM-1020
|
iGluR
|
Neurological Disease
|
Blixeprodil (GM-1020) is the orally active antagonist for NMDA receptor with an affinity of Ki=3.25 µM in rat cortical tissue. Blixeprodil inhibits NR1/2A-NMDAR-mediated currents in HEK293 cell with IC50 of 1.192 µM. Blixeprodil exhibits antidepressant in rats models. Blixeprodil can cross blood-brain barrier .
|
-
- HY-P3355
-
|
iGluR
|
Neurological Disease
|
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-119530
-
BW 57-323
|
Nucleoside Antimetabolite/Analog
|
Others
|
Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-124051
-
|
Elastase
|
Cardiovascular Disease
Inflammation/Immunology
|
BAY-8040 is a pyrimidopyridazine derivative which has inhibitory activity against human neutrophil elastase (HNE). BAY-8040 decreases cardiac remodeling and ameliorates cardiac function in a Monocrotaline (HY-N0750)-induced rat model for pulmonary arterial hypertension. BAY-8040 is promising for research of inflammatory pathologies and cardiopulmonary pathologies .
|
-
- HY-P990148
-
|
VEGFR
|
Cancer
|
Anti-Mouse VEGF-A Antibody (2G11-2A05) is a rat-derived IgG2a κ type antibody inhibitor, tragrting to mouse VEGF-A with high affinity. Anti-Mouse VEGF-A Antibody (2G11-2A05) shows good anti-tumor effect in gastric cancer xenograft models .
|
-
- HY-148195
-
NNZ-2591
|
Biochemical Assay Reagents
|
Neurological Disease
|
Ercanetide (NNZ 2591) is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). Ercanetide shows orally active and cross the blood-brain barrier. Ercanetide shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. Ercanetide has the potential for the research of ischemic brain injury and angelman syndrome .
|
-
- HY-158374
-
|
IRAK
|
Inflammation/Immunology
|
BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7 .
|
-
- HY-128932
-
MT-141
|
Antibiotic
Bacterial
PPAR
Prostaglandin Receptor
PTEN
Akt
mTOR
|
Infection
Cardiovascular Disease
Endocrinology
|
Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits antibacterial activity. Cefminox sodium is a broad-spectrum, bactericidal cephalosporin antibiotic. Cefminox sodium also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ. Cefminox sodium upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium also prevents pulmonary arterial hypertension in rat model .
|
-
- HY-147927
-
|
Enteropeptidase
|
Metabolic Disease
|
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research .
|
-
- HY-P5874
-
|
Calcium Channel
|
Inflammation/Immunology
|
Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .
|
-
- HY-15056
-
|
TRP Channel
|
Inflammation/Immunology
|
AMG 9090 is characterized as a compound that acts as a partial agonist of rat TRPA1 channels, demonstrating pharmacological activity in pain and inflammation models. TRPA1 is pivotal in sensing reactive compounds, triggering pain responses in humans and rodents. AMG 9090, along with other trichloro(sulfanyl)ethyl benzamides (TCEB compounds), shows differential effects on human and rat TRPA1 channels: it acts as a potent antagonist of human TRPA1 activated by AITC and noxious cold, whereas it behaves as a partial agonist at rat TRPA1. This suggests AMG 9090's potential as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory activity against TRPM8 noted .
|
-
- HY-109968A
-
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-109968
-
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-123187
-
|
JAK
|
Cardiovascular Disease
|
AS2553627 is a type of JAK inhibitor, with IC50 values of 0.46, 0.30, 0.14, and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively. AS2553627 can inhibit the proliferation of human and rat T cells stimulated by IL-2, with IC50 values of 2.4 and 4.3 nM, respectively. AS2553627 can reduce cardiac allograft vasculopathy and fibrosis in a rat heart transplant model, effectively extending survival rates. AS2553627 can be used to prevent acute and chronic rejection in heart transplants .
|
-
- HY-117991
-
|
VEGFR
|
Cancer
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-108467
-
GGsTop
5 Publications Verification
Nahlsgen
|
γ-Glutamyl Transferase (GGT)
|
Cardiovascular Disease
|
GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ-GGT inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150 and 51 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model .
|
-
- HY-P10360
-
|
α-synuclein
|
Neurological Disease
|
Tat-βsyn-degron is an α-synuclein knockdown peptide that effectively degrades α-synuclein protein via the proteasome pathway. Tat-βsyn-degron effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In a Parkinson's mouse toxicity model, Tat-βsyn-degron can alleviate parkinsonian toxin-induced neuronal damage and movement disorders .
|
-
- HY-111066
-
|
Dopamine Receptor
|
Others
|
JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
|
-
- HY-158013A
-
|
Dopamine Transporter
|
Neurological Disease
|
JJC8-088 dioxalate is the dioxalate salt form of JJC8-088 (HY-158013). JJC8-088 dioxalate is a derivative of modafinil. JJC8-088 dioxalate is an inhibitor for dopamine transporter (DAT). JJC8-088 dioxalate exhibits behavioral characteristics similar to cocaine in rat models, and can be to study psychostimulant use disorders .
|
-
- HY-N0665
-
(8E)-Nuezhenide
|
NF-κB
Wnt
|
Inflammation/Immunology
|
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of?Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA) .
|
-
- HY-W414915
-
CGP 48933 methyl ester
|
Angiotensin Receptor
|
Cardiovascular Disease
|
Valsartan methyl ester (Compound 3) is a derivative of Valsartan (HY-18204). Valsartan methyl ester is an orally active antagonist for angiotensin II, that inhibits angiotensin II (IC50 of 0.06 μM), angiotensin II-induced pressor response in rabbit aorta (IC50 of 0.068 μM) and angiotensin II-induced pressor response in the pithed rat model (10% inhibition at 10 mg/kg, p.o.) .
|
-
- HY-P11111
-
|
Drug Derivative
|
Others
|
QP5 is an Amelogenin (HY-P71627)-derived peptide. QP5 binds on the hydroxyapatite and demineralized tooth enamel surfaces, transitorily stabilize the amorphous calcium phosphate (ACP), control the crystallization of hydroxyapatite and promote the remineralization of caries lesions. QP5 promotes remineralization in rat caries models. QP5 can be used for oral diseases like dental caries research .
|
-
- HY-171472
-
|
Dopamine Receptor
|
Neurological Disease
|
A-86929 is a highly potent and selective dopamine D1 receptor agonist with a pKi value of 7.3. In the 6-OHDA (HY-B1081)-induced unilateral nigrostriatal lesion rat model, A-86929 significantly induces rotational behavior. It also improves motor function in the MPTP (HY-15608)-induced Parkinson's disease marmoset model. Additionally, A-86929 demonstrates potential therapeutic value in reducing cocaine-seeking behavior in rats and reversing Haloperidol (HY-14538)-induced cognitive deficits in rhesus monkeys. A-86929 can be used for research in neurological disorders .
|
-
- HY-162641
-
|
IRAK
NF-κB
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models .
|
-
- HY-163378
-
|
Complement System
|
Inflammation/Immunology
|
C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases .
|
-
- HY-120714
-
16091 RP
|
Others
|
Inflammation/Immunology
|
Metiazinic acid (16091 RP) is an anti-inflammatory agent. Metiazinic acid can be used for study of inflammation .
|
-
- HY-120476
-
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
JNJ-39729209 is an antagonist for transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.9, 8.5, 7.9 and 7.7 for TRPV1 from human, rat, canine and guinea pig. JNJ-39729209 inhibits Capsaicin (HY-10448)-induced hypotension and inhibit thereby hypothermia. JNJ-39729209 exhibits anti-inflammatory and analgesic activities in Carrageenan (HY-125474)- and CFA (HY-153808)-induced thermal hyperalgesia rat models. JNJ-39729209 exhibits anti-cough effects in guinea pigs .
|
-
- HY-13954
-
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
|
-
- HY-103552
-
|
mGluR
|
Neurological Disease
|
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
|
-
- HY-W415753
-
VUFB-15754
|
Drug Derivative
|
Neurological Disease
Inflammation/Immunology
|
Alaptide, a spirocyclic synthetic dipeptide and a derivative of melanocyte-stimulating hormone release-inhibiting factor (MIF), is a transdermal permeation modifier. Alaptide loaded on nanofibrous membranes accelerates the healing of skin incisions, particularly the healing of skin burns.
Alaptide is a nootropic agent, that influences the dopaminergic system and increases homovanillic acid level in the striatum of rat models. Alaptide can be used for wound healing with large damaged areas and neurological diseases research .
|
-
- HY-14895
-
CM346
|
Parasite
Monoamine Oxidase
Sigma Receptor
P-glycoprotein
|
Infection
Cardiovascular Disease
Neurological Disease
|
Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects .
|
-
- HY-122255
-
|
mGluR
|
Neurological Disease
|
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
|
-
- HY-144456
-
|
Xanthine Oxidase
|
Metabolic Disease
|
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model .
|
-
- HY-160602
-
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
CPL207280 is an orally active GPR40/FFA1 agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes .
|
-
- HY-118156
-
|
Others
|
Others
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
|
-
- HY-176274
-
-
- HY-N2995
-
Poricoic acid A(F)
|
NF-κB
Keap1-Nrf2
AMPK
TGF-beta/Smad
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
Poricoic acid A can be isolated from Poria cocos. Poricoic acid A is an orally active anti-tumor agent. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis. Poricoic acid A also attenuatea fibroblast activation and abnormal extracellular matrix remodeling in renal fibrosis by activating AMPK and inhibiting Smad3. Poricoic acid A significantly reduces the magnitude of rise in serum creatinine and urea levels in rat model when combined with Melatonin. Poricoic acid A ameliorates renal fibrosis and podocyte injury by attenuating oxidative stress and inflammation through regulating NF-κB and Nrf2 in IRI rodent model in combination with Melatonin .
|
-
- HY-W018026
-
L-p-Hydroxyphenylglycine; 4-Hydroxy-L-phenylglycine; UK 25842
|
Acyltransferase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
|
Oxfenicine (L-p-Hydroxyphenylglycine) is an orally active carnitine palmitoyltransferase-1 inhibitor. Oxfenicine inhibits the oxidation of fatty acids in the heart, protecting cardiac tissue from necrotic damage during ischemia, and also has an inhibitory effect on cardiac tissue apoptosis. In addition, Oxfenicine promotes lipolysis in a high-fat diet rat model. Oxfenicine can be used in the study of cardiovascular and metabolic diseases .
|
-
- HY-P1098
-
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
Ac2-26 is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-W700639
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
Tolafentrine, a dual-selective phosphodiesterase 3/4 (PDE3/4) inhibitor, has been shown to have significant acute and chronic effects in a unilateral diacetamide-induced rat pulmonary hypertension model. Experiments show that long-term administration can significantly alleviate all unilateral bisacetamide-induced hemodynamic and gas exchange abnormalities, reduce right ventricular hypertrophy, and normalize pulmonary vascular remodeling changes .
|
-
- HY-P1098A
-
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
Ac2-26 TFA is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-W931056
-
|
TRP Channel
|
Neurological Disease
|
AMG-628 is an orally active inhibitor for TRPV1, that inhibits Capsaicin (HY-10448) or acid (pH 5)-induced Ca 2+ influx into TRPV1- expressing CHO cell with IC50 of 4.9 and 3.1 nM. AMG-628 exhibits analgesic activity in Capsaicin (HY-10448)-induced rat model, and exhibits a half-life of 2.4 h in rats .
|
-
- HY-153968
-
|
Xanthine Oxidase
URAT1
|
Metabolic Disease
|
URAT1&XO inhibitor 1 (compound 29) is a dual inhibitor of both URAT1 (IC50=~10 μM) and Xanthine Oxidase (IC50=1.01 μM). URAT1&XO inhibitor 1 results hypouricemic effect in potassium oxonate-induced hyperuricemia rat model. URAT1&XO inhibitor 1 is used for hyperuricemia research .
|
-
- HY-100840A
-
4-Carboxy-3-hydroxyphenylglycine
|
mGluR
|
Neurological Disease
|
(RS)-4C3HPG (4-Carboxy-3-hydroxyphenylglycine) is an effective competitive antagonist at the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system, and it is also an agonist at mGluR2/3. (RS)-4C3HPG exhibits neuroprotective effects in an acute global ischemia rat model .
|
-
- HY-P990257
-
|
c-Fms
|
Cancer
|
Anti-Mouse CSF1 Antibody (5A1) is a rat-derived anti-mouse CSF1 IgG1 κ type antibody inhibitor. Anti-Mouse CSF1 Antibody (5A1) can inhibit cells proliferation and macrophage-induced invasion. Anti-Mouse CSF1 Antibody (5A1) shows potent anti-tumor effect in various tumor models, such as neuroblastoma .
|
-
- HY-B0596
-
TA-0910
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-155238
-
|
GABA Receptor
|
Neurological Disease
|
E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
|
-
- HY-121856
-
|
Others
|
Inflammation/Immunology
|
Flumizole, a derivative of substituted 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles, was synthesized and evaluated for its immunoregulatory and anti-inflammatory properties in animal models such as rat adjuvant-induced arthritis and mouse oxazolone-induced contact sensitivity assays. This compound class combines structural elements from flumizole and levamisole, aiming to enhance therapeutic efficacy. Symmetrically substituted 5,6-diaryl compounds with specific alkyl heteroatom or halogen substitutions showed optimal potency in the arthritis model. However, variations in activity were less consistent in the contact sensitivity assay. Flumizole and related compounds demonstrate potential as dual-action agents, targeting inflammation and immune modulation, offering promise for therapeutic development in immune-related disorders .
|
-
- HY-145607
-
-
- HY-176234
-
-
- HY-B0130R
-
|
Angiotensin-converting Enzyme (ACE)
NF-κB
STAT
Sirtuin
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Perindopril (Standard) is the analytical standard of Perindopril. This product is intended for research and analytical applications. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension .
|
-
- HY-10456
-
TAK-715
Maximum Cited Publications
13 Publications Verification
|
p38 MAPK
Casein Kinase
Wnt
|
Inflammation/Immunology
|
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
|
-
- HY-120485
-
IRFI-016
|
p38 MAPK
ERK
PKC
|
Cardiovascular Disease
|
Raxofelast (IRFI-016) is an antioxidant agent in various models of ischemia-reperfusion injury. Raxofelast has antiproliferative activity in H2O2-stimulated rat aortic smooth muscle cells. Raxofelast attenuates the activation of mitogen-activating protein kinase (MAPK), ERK kinase 1, 2 (MEK1,2) and protein kinase C (PKC) without affecting Ras expression .
|
-
- HY-170586
-
-
- HY-167715
-
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Traxanox is an orally available diuretic that enhances phagocytosis of yeast granules by mouse peritoneal macrophages and rat peritoneal polymorphonuclear leukocytes in vitro.
Traxanox inhibits IgE-mediated histamine release and cyclic AMP phosphodiesterase
activity.Traxanox exhibits anti-inflammatory activity, as it inhibits the anaphylactoid reaction and reduces pleural fluid accumulation in experimental models of inflammation. Traxanox also demonstrates a synergistic effect when combined with hydrocortisone or indomethacin in suppressing adjuvant arthritis in rats.
|
-
- HY-173503
-
|
GLUT
|
Metabolic Disease
|
DS-1150b is an orally active GLUT4 activator. DS-1150b has the activity of activating GLUT4 transport and can promote the translocation of GLUT4 to the cell membrane in skeletal muscle cells. DS-1150b has shown hypoglycemic effects in the Zucker obese rat model and can be used in the study of type 2 diabetes mellitus (T2DM) .
|
-
- HY-N0321
-
trans-Caftaric acid
|
Others
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
Caftaric acid (trans-Caftaric acid) is a polyphenolic antidiuretic, antioxidant and anti-apoptotic agent that can be hydrolyzed by intestinal microbial esterases. Caftaric acid exerts its antioxidant and potential anti-inflammatory effects mainly through intestinal microbial metabolism. Caftaric acid can reduce renal damage, restore electrolyte balance, renal function indicators and antioxidant enzyme activities in a rat albinism model, and further exert anti-oxidative stress and anti-inflammatory activities .
|
-
- HY-P3354
-
|
iGluR
|
Neurological Disease
|
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-132610A
-
ALN-AS1 sodium
|
Small Interfering RNA (siRNA)
|
Metabolic Disease
|
Givosiran (ALN-AS1) sodium is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran sodium downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran sodium demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran sodium can be used for the research of acute hepatic porphyria (AHP) .
|
-
- HY-147428
-
MM-110; (±)-18-Methoxycoronaridine
|
nAChR
Parasite
|
Infection
Neurological Disease
|
Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse . Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis .
|
-
- HY-162640
-
|
ROR
|
Cancer
|
LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-132610
-
ALN-AS1
|
Small Interfering RNA (siRNA)
|
Metabolic Disease
|
Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran can be used for the research of acute hepatic porphyria (AHP) .
|
-
- HY-145814
-
|
HSP
Fungal
|
Infection
|
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2) .
|
-
- HY-115566
-
|
LPL Receptor
Smo
|
Inflammation/Immunology
|
S1PL-IN-31 (compound ) is an oral active sphingosine-1-phosphate (S1P) lyase inhibitor with the IC50 of 210 nM. S1PL-IN-31 is Smoothened receptor antagonist with the IC50 of 440 nM. S1PL-IN-31 can be used for study of experimental autoimmune encephalomyelitis .
|
-
- HY-U00237B
-
|
Adrenergic Receptor
|
Others
|
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
|
-
- HY-W015815
-
|
Endogenous Metabolite
|
Neurological Disease
|
6-Methylnicotinamide is a nicotinamide derivative. 6-methylnicotinamide is also an endogenous metabolite and its sudden increase in the acute stages of intracerebral hemorrhage (ICH) exacerbates neurological damages in rat model. 6-Methylnicotinamide can significantly enhance the coordination effect between acylamino and undercoordinated defective Pb 2+ cations. 6-Methylnicotinamide results in enhanced efficiency of perovskite solar cells to 24.33% with excellent environmental storage, heat, and light stabilities .
|
-
- HY-P990264
-
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
Anti-Mouse CD70 Antibody (FR70) is a rat-derived ant-mouse CD70 IgG2b κ type antibody inhibitor. Anti-Mouse CD70 Antibody (FR70) decreases CD4 +, CD8 + T cells and eosinophils. Anti-Mouse CD70 Antibody (FR70) shows potent anti-inflammatory and anti-immune effects on allergic lung inflammation and cardiac transplant mice models .
|
-
- HY-W028142
-
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research .
|
-
- HY-12119B
-
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
GW274150 (dihydrochloride) is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 (dihydrochloride) displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 (dihydrochloride) exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-114873
-
LY25684
|
Phospholipase
COX
Lipoxygenase
Leukotriene Receptor
|
Inflammation/Immunology
|
LY256548 (LY25648) is an orally available anti-ischemic and anti-inflammatory compound with central nervous system activity. LY256548 is an inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and COX, and inhibits A23187 (HY-N6687)-stimulated leukotriene B4 production. LY256548 inhibits bone damage and paw swelling in the rat Freund's complete adjuvant-induced arthritis (FCA) model .
|
-
- HY-119821R
-
|
Reference Standards
Glycosidase
|
Infection
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-117133
-
SF0166
|
Integrin
|
Metabolic Disease
|
Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
|
-
- HY-N0665R
-
(8E)-Nuezhenide (Standard)
|
Reference Standards
NF-κB
Wnt
|
Inflammation/Immunology
|
Specnuezhenide (Standard) is the analytical standard of Specnuezhenide. This product is intended for research and analytical applications. Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of?Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA) .
|
-
- HY-17444
-
|
PPAR
|
Metabolic Disease
Cancer
|
Tesaglitazar is a dual-target PPARα/γ agonist with an EC50 of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain .
|
-
- HY-125064
-
|
Src
|
Cancer
|
AP22408 is a nonpeptide inhibitor against Src SH2 with an IC50 value of 0.3 μM. AP22408 inhibits rabbit osteoclast-mediated resorption of dentine, exhibits bone-targeting properties based on a hydroxyapatite adsorption assay and demonstrates in vivo antiresorptive activity in a parathyroid hormone-induced rat model. AP22408 is proming for rasearch of osteoporosis and other bone-related diseases such as Paget’s disease, osteolytic bone metastasis and hypercalcemia associated with malignancy .
|
-
- HY-12119
-
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-137307
-
(22S)-Hydroxycholesterol
|
LXR
ATP-binding cassette (ABC) transporters
|
Inflammation/Immunology
|
Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models .
|
-
- HY-115861
-
|
Endogenous Metabolite
|
Neurological Disease
|
UCM765 is a selective MT2-type melatonin receptor ligand with hypnotic, analgesic and anxiolytic activities. The partial agonist effect of UCM765 has attracted attention in pharmacological studies. By structurally modifying UCM765, its water solubility and metabolic stability can be improved, thereby increasing its bioavailability. The biological activity of UCM765 has been verified in a rat model, supporting its potential for further pharmacological studies .
|
-
- HY-W747879
-
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
Diclofenac Amide- 13C6 is the 13C-labeled Diclofenac amide (HY-134521). Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
|
-
- HY-B0130S1
-
-
- HY-Y0546
-
|
Endogenous Metabolite
Photosensitizer
|
Cancer
|
Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-12119A
-
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-11052A
-
|
Opioid Receptor
|
Neurological Disease
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
|
-
- HY-W028142R
-
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research .
|
-
- HY-119530R
-
BW 57-323 (Standard)
|
Nucleoside Antimetabolite/Analog
Reference Standards
|
Others
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-169986S
-
|
JAK
|
Inflammation/Immunology
|
TyK2-IN-21-d3 (Compound 3c) is the orally active prodrug of the tyrosine kinase 2. TyK2-IN-21-d3 exhibits good chemical stability in aqueous system under different pHs. TyK2-IN-21-d3 alleviates the effect of gastric acid changes on drug absorption and improve the drug bioavailability in rat model .
|
-
- HY-162639
-
|
Glycosidase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
α-Glucosidase-IN-68 (Compound 2) is an inhibitor for α-Glucosidase, AChE, and BChE, with IC50 of 0.251, 0.774 and 0.793 μM, respectively. α-Glucosidase-IN-68 exhibits antioxidant efficacy, with IC50 of 0.69 μM and 0.02 μM, in DPPH and ABTS experiments. α-Glucosidase-IN-68 exhibits antidiabetic effect in Streptozotocin (HY-13753)-induced diabetic rat models .
|
-
- HY-113427R
-
|
Endogenous Metabolite
Reference Standards
Bcl-2 Family
Apoptosis
|
Cardiovascular Disease
Cancer
|
trans-Vaccenic acid (Standard) is the analytical standard of trans-Vaccenic acid (HY-113427). This product is intended for research and analytical applications. trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity.
|
-
- HY-128932R
-
MT-141 (Standard)
|
Reference Standards
Antibiotic
Bacterial
PPAR
Prostaglandin Receptor
PTEN
Akt
mTOR
|
Infection
Cardiovascular Disease
Endocrinology
|
Cefminox (sodium) (MT-141) (Standard) is the analytical standard of Cefminox (sodium). This product is intended for research and analytical applications. Cefminox sodium is a semisynthetic cephamycin, which exhibits antibacterial activity. Cefminox sodium is a broad-spectrum, bactericidal cephalosporin antibiotic. Cefminox sodium also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ. Cefminox sodium upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium also prevents pulmonary arterial hypertension in rat model .
|
-
- HY-W015815R
-
|
Endogenous Metabolite
|
Neurological Disease
|
6-Methylnicotinamide is a nicotinamide derivative. 6-methylnicotinamide is also an endogenous metabolite and its sudden increase in the acute stages of intracerebral hemorrhage (ICH) exacerbates neurological damages in rat model. 6-Methylnicotinamide can significantly enhance the coordination effect between acylamino and undercoordinated defective Pb2+ cations. 6-Methylnicotinamide results in enhanced efficiency of perovskite solar cells to 24.33% with excellent environmental storage, heat, and light stabilities .
|
-
- HY-113427S
-
|
Isotope-Labeled Compounds
Endogenous Metabolite
Bcl-2 Family
Apoptosis
|
Cardiovascular Disease
Cancer
|
trans-Vaccenic acid-d13 is deuterium labeled trans-Vaccenic acid (HY-113427). trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
|
-
- HY-P1098B
-
|
IKK
|
Inflammation/Immunology
|
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-10932
-
Ro 13-5057
|
nAChR
iGluR
|
Neurological Disease
|
Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
|
-
- HY-10281
-
|
Factor Xa
|
Cardiovascular Disease
|
YM-60828 is an FXa inhibitor with antithrombotic properties. In the rat arteriovenous shunt model, YM-60828 does not prolong coagulation time but reduces the levels of thrombin-antithrombin III complex (TAT) in a dose-dependent manner. YM-60828 exhibits only anti-FXa activity and does not show anti-thrombin activity, indicating that its antithrombotic effect is independent of thrombin. Therefore, the antithrombotic effect of YM-60828 can be monitored by TAT .
|
-
- HY-162710
-
|
Aminopeptidase
|
Inflammation/Immunology
|
LTA4H-IN-5 (Compound H122) is an orally active inhibitor for leukotriene A4 hydrolase (LTA4H), that inhibits the LTA4H aminopeptidase and LTA4H hydrolase with IC50 of 0.38 nM and 16.93 nM. LTA4H-IN-5 exhibits good pharmacokinetic characteristics in C57 mice and ameliorates the DNBS-induced ulcerative enteritis in rat models .
|
-
- HY-10819
-
|
Antifolate
|
Cancer
|
AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a Km of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED .
|
-
- HY-124517
-
|
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
Inflammation/Immunology
|
Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768) .
|
-
- HY-163538
-
|
PI3K
Apoptosis
|
Cancer
|
TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
|
-
- HY-B0596A
-
TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-P99171
-
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
- HY-169404
-
|
PPAR
|
Metabolic Disease
|
PPARγ agonist 15 (Compound 7c) is an agonist for PPARγ. PPARγ agonist 15 inhibits the expression of alpha-amylase (HPA) and alpha-glucosidase (HLAG) with IC50 of 28.35 µM and 26.21 µM. PPARγ agonist 15 enhances glucose uptake in the L6 myotube cell. PPARγ agonist 15 improves glucose homeostasis, insulin sensitivity, and lipid metabolism in rat Streptozotocin (HY-13753)-induced diabetes model .
|
-
- HY-137555
-
11-dehydro-2,3-dinor TXB2
|
Endogenous Metabolite
|
Metabolic Disease
|
11-dehydro-2,3-dinor Thromboxane B2 (11-dehydro-2,3-dinor TXB2) is a metabolite of the TXA2 inactive metabolite TXB2 (Item No. 19030). It is formed from TXB2 by cytosolic aldehyde dehydrogenase (ALDH) and β-oxidation. Levels of 11-dehydro-2,3-dinor TXB2 are increased 5.2-fold in a surgery-induced rat model of tendon overuse.
|
-
- HY-B1350A
-
Sodium fusidate; SQ-16360
|
Bacterial
Antibiotic
Interleukin Related
|
Infection
Inflammation/Immunology
|
Fusidic acid sodium salt is an orally available antibacterial agent that inhibits bacterial protein synthesis by preventing the release of translation elongation factor G (EF-G) from ribosomes. Fusidic acid sodium salt inhibits the inhibitory and activating effects of interleukins IL-1 and IL-6 on glucose-induced insulin production and exhibits antidiabetic effects in a rat model. Fusidic acid sodium salt improves the symptoms of colitis in rats and inhibits the growth of Toxoplasma gondii and Listeria monocytogenes EGD in vitro, but not in mice .
|
-
- HY-111164
-
|
p38 MAPK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 with anti-inflammatory and anti-allodynic activities. CBS-3595 reduces the production of the proinflammatory cytokine IL-6 and increases the levels of the anti-inflammatory cytokine IL-10 in rats. CBS-3595 reduces paw oedema formation in the Complete Freund’s adjuvant (CFA) (HY-153808)-induced arthritis rat model. CBS-3595 is promising for research of autoimmune diseases .
|
-
- HY-169940
-
|
HDAC
|
Inflammation/Immunology
|
Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by inhibiting HDAC6 activity, with an IC50 value of 63 nM. It also exhibits good selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat significantly downregulates fibrotic markers (fibronectin and collagen 1) in fibroblasts. Additionally, Fibrostat demonstrated no toxicity in rat-perfused heart and zebrafish larvae models. Fibrostat shows potential for research into fibrosis-related diseases .
|
-
- HY-109106A
-
SK-1403; AJT240; PLS240
|
CaSR
|
Endocrinology
|
Upacicalcet sodium is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet sodium reduces serum intact parathyroid hormone (iPTH) and serum Ca 2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet sodium sodium improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet sodium sodium inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet sodium is useful for studying SHPT .
|
-
- HY-108467R
-
|
γ-Glutamyl Transferase (GGT)
|
Cardiovascular Disease
|
GGsTop (Standard) is the analytical standard of GGsTop. This product is intended for research and analytical applications. GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ-GGT inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150 and 51 M-1 s-1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model .
|
-
- HY-109106
-
SK-1403 free acid; AJT240 free acid; PLS240 free acid
|
CaSR
|
Endocrinology
|
Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet is useful for studying SHPT .
|
-
- HY-101046
-
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research .
|
-
- HY-W414915R
-
CGP 48933 methyl ester (Standard)
|
Reference Standards
Angiotensin Receptor
|
Cardiovascular Disease
|
Valsartan methyl ester (Standard) is the analytical standard of Valsartan methyl ester. This product is intended for research and analytical applications. Valsartan methyl ester (Compound 3) is a derivative of Valsartan (HY-18204). Valsartan methyl ester is an orally active antagonist for angiotensin II, that inhibits angiotensin II (IC50 of 0.06 μM), angiotensin II-induced pressor response in rabbit aorta (IC50 of 0.068 μM) and angiotensin II-induced pressor response in the pithed rat model (10% inhibition at 10 mg/kg, p.o.) .
|
-
- HY-169332
-
|
Piezo Channel
ERK
|
Metabolic Disease
|
Piezo1 agonist 1-d2 (Compound 12a) is an agonist for Piezo1 with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates the Ca 2+-related ERK signaling pathway, and thus promotes the osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs). Piezo1 agonist 1-d2 ameliorates disuse osteoporosis in the hindlimb-unloading (HU) rat model .
|
-
- HY-P99124
-
|
CD3
|
Inflammation/Immunology
|
Anti-Mouse CD3 Antibody (17A2) is an anti-mouse CD3 IgG2b antibody inhibitor derived from the host Rat. Anti-Mouse CD3 Antibody (17A2) enhances T-cell proliferation and activation and stimulate IFN-γ or IL-17 production in splenic T cells. Anti-Mouse CD3 Antibody (17A2) significantly suppresses mortality in Graft-versus-host disease (GVHD) mice models .
|
-
- HY-162347
-
|
Sodium Channel
|
Neurological Disease
|
Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that significantly inhibits Veratridine (HY-N6691)-induced neuronal activity. Nav1.7-IN-13 inhibits total Na+ current in DRG neurons in a concentration-dependent manner; slows down the activation of Navs. Nav1.7-IN-13 significantly alleviated mechanical pain behavior in a rat model of nerve injury (SNI) and had analgesic activity .
|
-
- HY-168333
-
|
5-HT Receptor
mTOR
CDK
|
Neurological Disease
|
5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL)-induced rat model .
|
-
- HY-19109
-
|
Leukotriene Receptor
|
Others
|
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
|
-
- HY-B1119
-
|
Bacterial
Fungal
Antibiotic
Apoptosis
|
Infection
Cancer
|
Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 µM and 10 µM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-Y0546S2
-
|
Isotope-Labeled Compounds
Endogenous Metabolite
Photosensitizer
|
Cancer
|
Benzophenone- 13C is the 13C labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-N2840
-
Allodulcitol
|
Bacterial
Drug Intermediate
|
Metabolic Disease
Cancer
|
Allitol is a rare natural polyol that can be used as a sweetener. Allitol is a sugar alcohol formed by linking D- and L-hexoses in a process called izumoring. Allitol has anti-diabetic effects in a long-term allitol diet rat model. Allitol significantly increases the phylum Bacillota and decreases the phyla Bacteroidetes Actinomycetota, and Pseudomonadota. Allitol significantly increases the levels of butyric acid-metabolizing enzymes in a PICRUSt2 gut microbiota analysis. Allitol is an important intermediate for the preparation of the agents which against diabetes, cancer, and viral infections, including AIDS .
|
-
- HY-100769
-
YL0919
|
5-HT Receptor
|
Neurological Disease
|
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .
|
-
- HY-118152
-
|
5-HT Receptor
|
Neurological Disease
|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively .Org-12962 displays antiaversive effects in a rat model of panic-like anxiety .
|
-
- HY-123468
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-123468A
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-171174
-
|
CDK
STAT
Wnt
|
Cancer
|
CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1 SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57% .
|
-
- HY-168096
-
|
NO Synthase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
iNOs-IN-5 (Compound BN-4) is an inhibitor for iNOS with an IC50 of 0.1707 μM, and reduces NO levels in LPS (HT-D1056)-induced RAW264.7 cells. iNOs-IN-5 reduces the hypoxic injury stimulated ROS and lactate dehydrogenase expression, and exhibits anti-necrosis and anti-apoptosis efficacy. iNOs-IN-5 exhibits anti-cerebral ischemia and neuroprotective activities in SD rat models. iNOs-IN-5 is blood-brain barrier penetrable .
|
-
- HY-Y0546S1
-
|
Isotope-Labeled Compounds
Endogenous Metabolite
Photosensitizer
|
Cancer
|
Benzophenone-d5 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-Y0546S
-
|
Isotope-Labeled Compounds
Endogenous Metabolite
Photosensitizer
|
Cancer
|
Benzophenone-d10 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-116062A
-
|
Histone Methyltransferase
|
Neurological Disease
|
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
|
-
- HY-10932R
-
Ro 13-5057 (Standard)
|
Reference Standards
nAChR
iGluR
|
Neurological Disease
|
Aniracetam (Standard) is the analytical standard of Aniracetam. This product is intended for research and analytical applications. Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
|
-
- HY-107428
-
|
MMP
|
Cardiovascular Disease
|
PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
|
-
- HY-109139
-
NIR178; PBF509
|
Adenosine Receptor
|
Neurological Disease
Cancer
|
Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response .
|
-
- HY-109106B
-
(Rac)-SK-1403 free acid; (Rac)-AJT240 free acid; (Rac)-PLS240 free acid
|
CaSR
|
Endocrinology
|
(Rac)-Upacicalcet is the racemate of Upacicalcet (HY-109106). Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet is useful for studying SHPT .
|
-
- HY-173221
-
|
NF-κB
p38 MAPK
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
MJ210 is a modulator of the NF-κB and MAPK pathways with oral activity and the ability to penetrate the blood-brain barrier, and it exhibits neuroprotective activity. In vitro, 5 μM of MJ210 can increase the survival rate of SH-SY5Y cells treated with Rotenone (HY-B1756) to 81.9% and reduce the level of ROS, etc. In vivo, 5 mg/kg of MJ210 can improve the motor impairment in a rat model of Parkinson's disease. MJ210 can be used in the research of neurological diseases, such as Parkinson's disease .
|
-
- HY-112348
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-100847
-
|
PARP
|
Cancer
|
AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models .
|
-
- HY-N0194
-
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-147927A
-
|
Enteropeptidase
|
Metabolic Disease
|
(S)-Human enteropeptidase-IN-1 (Compound 6c) is an orally active enteropeptidase inhibitor with low systemic exposure (IC50 (initial): 26 nM; IC50 (app): 1.8 nM). (S)-Human enteropeptidase-IN-1 promotes increased fecal protein output and effectively reduces body weight in a diet-induced obese (DIO) rat model. (S)-Human enteropeptidase-IN-1 inhibits enteropeptidase via a reversible covalent mechanism and prolongs the enzyme inactivation time. (S)-Human enteropeptidase-IN-1 can be used in anti-obesity research .
|
-
- HY-107513
-
|
mGluR
|
Neurological Disease
Cancer
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
|
-
- HY-P10587
-
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
|
Inflammation/Immunology
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. In addition, Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-176214
-
|
PPAR
COX
|
Metabolic Disease
|
PPARγ agonist 19 (Compound 5e) is a PPARγ agonist. PPARγ agonist 19 has an IC50 of 11.27 μM against COX-1 and an IC50 of 0.05 μM against COX-1. PPARγ agonist 19 increases glucose uptake in rat hemidiaphragm assay and is superior to pioglitazone (HY-13956). PPARγ agonist 19 alleviates hyperglycemia and insulin resistance in an in vivo model of type 2 diabetes in rats and protects against renal and lipidemia damage caused by metabolic dysfunction .
|
-
- HY-Y0546R
-
|
Reference Standards
Endogenous Metabolite
Photosensitizer
|
Cancer
|
Benzophenone (Standard) is the analytical standard of Benzophenone. This product is intended for research and analytical applications. Benzophenone standard is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone standard can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone standard can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone standard exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone standard exhibits estrogenic activity .
|
-
- HY-19210
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
|
-
- HY-111140
-
|
PGE synthase
Lipoxygenase
PPAR
|
Inflammation/Immunology
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) . YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells . YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) . YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research .
|
-
- HY-B0340
-
DM9384; DZL-221
|
nAChR
iGluR
mGluR
PKC
GABA Receptor
Calcium Channel
|
Neurological Disease
|
Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca 2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research .
|
-
- HY-N4107
-
|
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-N4107R
-
|
Reference Standards
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-172236
-
BNC210; IW-2143
|
nAChR
|
Neurological Disease
|
Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 (HY-12560A) with IC50 values in the range of 1.2 to 3 μM. Soclenicant can be used in studies of anxiety, trauma, and stressor-related disorders .
|
-
- HY-173488
-
|
NF-κB
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
|
Cancer
|
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
|
-
- HY-15495B
-
(3S)-CC-930 hydrochloride
|
JNK
ERK
p38 MAPK
EGFR
TNF Receptor
|
Inflammation/Immunology
|
(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC50 values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC50 = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research .
|
-
- HY-W653962
-
|
Isotope-Labeled Compounds
Apoptosis
Antibiotic
Fungal
Bacterial
|
Infection
Cancer
|
Triclosan- 13C6 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-158223
-
CMCSMA
|
Biochemical Assay Reagents
|
Others
|
Carboxymethyl chitosan Methacryloyl (CMCSMA) is methacrylated carboxymethyl chitosan with properties as a 3D printing ink. A composite hydrogel made of Carboxymethyl chitosan Methacryloyl can effectively accelerate bone healing in an infectious microenvironment after implantation in a rat model of Staphylococcus aureus-infected femoral defect . Carboxymethyl chitosan Methacryloyl needs to self-assemble into fibrous hydrogel under the action of photoinitiator LAP (HY-44076), and target bioactive adhesion sites, play an inherent supporting role for tissue cells and biodegradable activity. Application: cell culture, biological 3D printing, tissue engineering, etc.
|
-
- HY-W747491
-
|
Isotope-Labeled Compounds
Antibiotic
Apoptosis
Bacterial
Fungal
|
Cancer
|
Triclosan- 13C12 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-B1119R
-
|
Reference Standards
Bacterial
Fungal
Antibiotic
Apoptosis
|
Infection
Cancer
|
Triclosan (Standard) is the analytical standard of Triclosan. This product is intended for research and analytical applications. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 µM and 10 µM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-155517
-
|
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
|
INF200 (compound 5) is a sulfonylurea-based inhibitor of NLRP3 and NLRP3-mediated pyroptosis. INF200 has beneficial cardiometabolic effects in rat model of high-fat diet (HFD)-induced metaflammation,and shows anti-inflammatory activity to (10 μM) decreases IL-1β release in human macrophages. INF200 improves glucose and lipid profiles,and attenuates systemic inflammation and biomarkers of cardiac dysfunction (particularly BNP). INF200 also improves myocardial damage-dependent ischemia/reperfusion injury (IRI) in hemodynamic evaluation .
|
-
- HY-175637
-
|
COX
MyD88
|
Neurological Disease
Inflammation/Immunology
|
COX-2-IN-57 is an orally active COX-2 inhibitor with an IC50 value of 0.02 μM. COX-2-IN-57 reduces MyD88 expression and decreases serum levels of COX-2, PGE2, and COX-1 in Cisplatin (HY-17394)/radiation-induced neuropathy rat model. COX-2-IN-57 demonstrates superior antinociceptive efficacy in hot plate, cold allodynia, and Randall-Selitto tests, along with hepato-/renal protection. COX-2-IN-57 can be used for the study of inflammation .
|
-
- HY-15048
-
|
PARP
|
Inflammation/Immunology
|
GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrated strong anti-inflammatory effects. It reduced inflammatory cell infiltration, histological injury, and delayed clinical signs of inflammation. GPI 15427 also diminished the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats. These results suggest GPI 15427 could be useful for treating intestinal ischemia and inflammation .
|
-
- HY-P10870
-
|
Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
|
Cancer
|
Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
|
-
- HY-173024
-
|
TRP Channel
|
Neurological Disease
|
TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
|
-
- HY-N0194R
-
|
Reference Standards
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-N2840R
-
Allodulcitol (Standard)
|
Reference Standards
Drug Intermediate
Bacterial
|
Metabolic Disease
Cancer
|
D-Tartaric acid (Standard) is the analytical standard of D-Tartaric acid. This product is intended for research and analytical applications. Allitol is a rare natural polyol that can be used as a sweetener. Allitol is a sugar alcohol formed by linking D- and L-hexoses in a process called izumoring. Allitol has anti-diabetic effects in a long-term allitol diet rat model. Allitol significantly increases the phylum Bacillota and decreases the phyla Bacteroidetes Actinomycetota, and Pseudomonadota. Allitol significantly increases the levels of butyric acid-metabolizing enzymes in a PICRUSt2 gut microbiota analysis. Allitol is an important intermediate for the preparation of the agents which against diabetes, cancer, and viral infections, including AIDS .
|
-
- HY-162677
-
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
|
-
- HY-P990259
-
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
- HY-17655
-
|
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
|
TBE56, a molecular glue, is a BACH1 degrader, with an EC50 of 44 nM. TBE56 is a weak NRF2 inducer and the biotinylated TBE31. TBE56 interacts and promotes the
degradation of BACH1 via a mechanism involving the E3 ligase FBX022. TBE56 reduces intracellular Fe 2+ accumulation, ROS generation, and malondialdehyde (MDA) content, while increasing GSH/GSSG ratio and upregulating GPX4 in Prominin-2-overexpressed BMSCs. TBE56 significantly ameliorates intervertebral disc degeneration (IVDD) in puncture-induced SD rat IVDD model. TBE56 can be used for the study of intervertebral disc degeneration (IVDD) .
|
-
- HY-116673
-
|
Histone Acetyltransferase
|
Neurological Disease
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
|
-
- HY-134160
-
5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
|
-
- HY-P990792
-
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
Anti-Mouse CD4 Antibody (GK1.5) is an anti-mouse CD4 IgG2b monoclonal antibody. Anti-Mouse CD4 Antibody (GK1.5) can significantly deplete CD4 + T cells. Anti-Mouse CD4 Antibody (GK1.5) can extend the survival rate of xenograft models. Anti-Mouse CD4 Antibody (GK1.5) can be used for research on immunology. The recommend isotype control of Anti-Mouse CD4 Antibody (GK1.5): Rat IgG2b kappa, Isotype Control (HY-P990682) .
|
-
- HY-175824
-
|
iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
|
-
- HY-W047432
-
DL0805
|
ROCK
|
Cardiovascular Disease
|
5-Nitro-1H-indazole-3-carbonitrile (DL0805) is a Rho kinase(ROCK) inhibitor with an IC50 of 6.67 μM for ROCK-I. 5-Nitro-1H-indazole-3-carbonitrile reduces Norepinephrine (HY-13715)-induced transient contraction and inhibits contraction induced by increasing external calcium in the endothelium-denuded rings of rat models. 5-Nitro-1H-indazole-3-carbonitrile has a vasorelaxant activity but high toxicity. 5-Nitro-1H-indazole-3-carbonitrile can be used for cardiovascular diseases, especially hypertension research .
|
-
- HY-116763
-
|
COX
LOX-1
|
|
COX-2/5-LOX-IN-4 (Compound 1) is a dual inhibitor that acts on both COX-2 and 5-LOX, with IC50 values of 0.05 μM for COX-2 and 0.003 μM for 5-LOX. By inhibiting the arachidonic acid metabolism pathway, COX-2/5-LOX-IN-4 reduces the production of prostaglandins and leukotrienes, alleviating inflammatory responses. In a rat ear edema model, intravenous administration (0.01 and 0.1 mg/kg) reduced edema by 41% and 44%, respectively, demonstrating significant anti-inflammatory effects. COX-2/5-LOX-IN-4 shows promise for studying the mechanisms of inflammatory diseases .
|
-
- HY-149454
-
|
P2Y Receptor
|
Cancer
|
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
|
-
- HY-151093
-
-
- HY-18071A
-
|
Na+/H+ Exchanger (NHE)
Autophagy
|
Cardiovascular Disease
|
BI-9627 hydrochloride is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride decreases autophagy in HTR-8/SVneo cells. BI-9627 hydrochloride can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 hydrochloride prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-100603A
-
|
PI3K
PI4K
|
Infection
|
(S)-GSK-F1 (Compound 28) is an inhibitor for type III phosphatidylinositol 4-kinase α (PI4KIIIα). (S)-GSK-F1 inhibits PI4Kα, PI4Kβ, PI4Kγ, PI3Kα, PI3Kβ and PI3Kδ with pIC50 of 8.3, 6.0, 5.6, 5.6, 5.1 and 5.6, respectively. (S)-GSK-F1 exhibits anti-hepatitis C virus (HCV) activity through inhibition of HCV replication. (S)-GSK-F1 exhibits moderate pharmacokinetic characters in rat model .
|
-
- HY-177277
-
|
PI3K
|
Inflammation/Immunology
|
HM5023507 is an orally active and selective PI3Kδ/γ inhibitor with IC50s of 4 and 5 μM for PI3Kδ and PI3Kγ over PI3Kβ and PI3Kα. HM5023507 attenuates the PI3Kδ/γ signaling in human basophils. HM5023507 also attenuates the activation and function of human B and T cells and cytokine and IgG production during cocultures, and Th17 differentiation of CD4 T cells. HM5023507 inhibited semiestablished collagen-induced arthritic inflammation in the rat models. HM5023507 can be used for inflammatory diseases like rheumatoid arthritis research .
|
-
- HY-N3847
-
Eriodictyol 7-O-β-D-glucoside
|
Keap1-Nrf2
|
Neurological Disease
|
Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is an Nrf2 activator. Eriodictyol-7-O-glucoside exhibits significant scavenging effects on both hydroxyl radicals and superoxide anions, with IC50 values of 0.28 mM and 0.30 mM, respectively. Eriodictyol-7-O-glucoside increases the nuclear localization of Nrf2 and induces the expression of the Nrf2/ARE-dependent genes. Eriodictyol-7-O-glucoside provides protection against oxygen and glucose deprivation (OGD)-induced oxidative insult. Eriodictyol-7-O-glucoside demonstrates neuroprotective efficacy in a rat model of focal cerebral ischemia (MCAO). Eriodictyol-7-O-glucoside can be used for the study of stroke .
|
-
- HY-W013403
-
|
IFNAR
|
Infection
|
2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
|
-
- HY-18071
-
BI-9627
2 Publications Verification
|
Na+/H+ Exchanger (NHE)
Autophagy
|
Cardiovascular Disease
|
BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-136805
-
|
Potassium Channel
|
Neurological Disease
|
Kv1.5-IN-1 is a Kv1.5 channel inhibitor. Its target selectivity and pharmacodynamic effects were evaluated in an in vitro rat model. After the introduction of a methoxy group at the R5 position, Kv1.5-IN-1 showed inhibitory potency similar to that of the unsubstituted compound. Its IC50 value for hKv1.5 channels was 0.51 μM. Kv1.5-IN-1 exhibited a high degree of selectivity, nearly 2,600 times higher than compound Ik and 300 times higher than compound IId, indicating that it may be a safe inhibitor. Due to its good pharmacological behavior, Kv1.5-IN-1 deserves further pharmacodynamic and pharmacokinetic evaluation. These properties make Kv1.5-IN-1 a potential Kv1.5 channel inhibitor that may have application prospects in the treatment of related diseases.
|
-
- HY-134160S
-
5-DHFU-13C,15N2; 5-Fluorodihydropyrimidine-2,4-dione-13C,15N2; 5-Fluorodihydrouracil-13C,15N2
|
Isotope-Labeled Compounds
Nucleoside Antimetabolite/Analog
|
Cancer
|
5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
|
-
- HY-N15378
-
|
IAP
Bcl-2 Family
COX
TNF Receptor
Caspase
Apoptosis
|
Inflammation/Immunology
Cancer
|
β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer .
|
-
- HY-12764R
-
-
- HY-12764
-
6-OAU
2 Publications Verification
GTPL5846
|
GPR84
ERK
Bacterial
Antibiotic
|
Inflammation/Immunology
|
6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC50 value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function .
|
-
- HY-W013403S
-
|
IFNAR
|
Infection
|
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
|
-
- HY-175340
-
|
Potassium Channel
TSPO
|
Neurological Disease
|
Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-Y0816
-
|
Biochemical Assay Reagents
|
(S)-Mandelic Acid is a (S)-enantiomer of Mandelic Acid (HY-W015591). (S)-Mandelic Acid undergoes one-directional chiral inversion to (R)-Mandelic Acid in rat models. (S)-Mandelic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
|
-
- HY-158223
-
CMCSMA
|
3D Bioprinting
|
Carboxymethyl chitosan Methacryloyl (CMCSMA) is methacrylated carboxymethyl chitosan with properties as a 3D printing ink. A composite hydrogel made of Carboxymethyl chitosan Methacryloyl can effectively accelerate bone healing in an infectious microenvironment after implantation in a rat model of Staphylococcus aureus-infected femoral defect . Carboxymethyl chitosan Methacryloyl needs to self-assemble into fibrous hydrogel under the action of photoinitiator LAP (HY-44076), and target bioactive adhesion sites, play an inherent supporting role for tissue cells and biodegradable activity. Application: cell culture, biological 3D printing, tissue engineering, etc.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1090
-
|
Cannabinoid Receptor
|
Neurological Disease
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1010
-
Z-LEHD-FMK
Maximum Cited Publications
13 Publications Verification
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-P3498
-
ZP1846
|
GCGR
|
Others
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model .
|
-
- HY-P11043
-
|
GLP Receptor
Neuropeptide Y Receptor
Arrestin
|
Metabolic Disease
|
GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
|
-
- HY-P5978
-
ANP 127-150 (Rat)
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
Atriopeptin III (ANP 127-150) (rat), a 24-amino acid atrial peptide, is a potent vasodilator and natriuretic/diuretic agent. Atriopeptin III (rat) improves renal functions and decreases blood pressure in a ureter-obstructed rat kidney model. Atriopeptin III (rat) can be used for research of chronic renal failure .
|
-
- HY-P1090A
-
|
Cannabinoid Receptor
|
Neurological Disease
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P10427
-
|
CXCR
HIV
|
Infection
|
DV1 is a selective antagonist for CXC chemokine receptor 4 (CXCR4). DV1 exhibits antiviral activity by blocking HIV-1 entry through the CXCR4 co-receptor. DV1 is stable in rat plasma and exhibits good pharmacokinetic characteristics in rat models .
|
-
- HY-P1010A
-
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-P3199
-
|
PKC
|
Inflammation/Immunology
|
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction .
|
-
- HY-P1694
-
|
Bradykinin Receptor
|
Cardiovascular Disease
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-P10580
-
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-P1091
-
|
Cannabinoid Receptor
|
Neurological Disease
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P10580A
-
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-12378
-
BQ-123
2 Publications Verification
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-P10898
-
-
- HY-119152
-
|
Insulin Receptor
Tyrosinase
Akt
|
Others
|
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model .
|
-
- HY-P1091A
-
|
Cannabinoid Receptor
|
Neurological Disease
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P10977
-
|
Sodium Channel
RIP kinase
|
Neurological Disease
|
Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease .
|
-
- HY-P11245
-
|
Amylin Receptor
|
Metabolic Disease
|
NN1213 (Peptide 21), a long-acting human amylin peptide analog, is a selective Amylin receptor agonist with an EC50 of 0.177 and 0.262 nM for hAMY3R and rAMY3R, respectively. NN1213 significantly reduces appetite in rat and dog models. NN1213 can be used for antiobesity research .
|
-
- HY-P11245A
-
|
Amylin Receptor
|
Metabolic Disease
|
NN1213 acetate (Peptide 21), a long-acting human amylin peptide analog, is a selective Amylin receptor agonist with an EC50 of 0.177 and 0.262 nM for hAMY3R and rAMY3R, respectively. NN1213 acetate significantly reduces appetite in rat and dog models. NN1213 acetate can be used for antiobesity research .
|
-
- HY-P3355
-
|
iGluR
|
Neurological Disease
|
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-148195
-
NNZ-2591
|
Biochemical Assay Reagents
|
Neurological Disease
|
Ercanetide (NNZ 2591) is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). Ercanetide shows orally active and cross the blood-brain barrier. Ercanetide shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. Ercanetide has the potential for the research of ischemic brain injury and angelman syndrome .
|
-
- HY-P5874
-
|
Calcium Channel
|
Inflammation/Immunology
|
Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .
|
-
- HY-P10360
-
|
α-synuclein
|
Neurological Disease
|
Tat-βsyn-degron is an α-synuclein knockdown peptide that effectively degrades α-synuclein protein via the proteasome pathway. Tat-βsyn-degron effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In a Parkinson's mouse toxicity model, Tat-βsyn-degron can alleviate parkinsonian toxin-induced neuronal damage and movement disorders .
|
-
- HY-P11111
-
|
Drug Derivative
|
Others
|
QP5 is an Amelogenin (HY-P71627)-derived peptide. QP5 binds on the hydroxyapatite and demineralized tooth enamel surfaces, transitorily stabilize the amorphous calcium phosphate (ACP), control the crystallization of hydroxyapatite and promote the remineralization of caries lesions. QP5 promotes remineralization in rat caries models. QP5 can be used for oral diseases like dental caries research .
|
-
- HY-P1098
-
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
Ac2-26 is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-P1098A
-
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
Ac2-26 TFA is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-P3354
-
|
iGluR
|
Neurological Disease
|
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-P1098B
-
|
IKK
|
Inflammation/Immunology
|
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-P10587
-
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
|
Inflammation/Immunology
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. In addition, Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-P10870
-
|
Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
|
Cancer
|
Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
|
-
- HY-175824
-
|
iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990302
-
|
nAChR
|
Neurological Disease
|
Anti-Human/Rat/Fish AChR Antibody (Mab35) is an anti-human/rat/fish AChR IgG1 monoclonal antibody. Anti-Human/Rat/Fish AChR Antibody (Mab35) can attack the AChR of neuromuscular junctions. Anti-Human/Rat/Fish AChR Antibody (Mab35) can be used for the construction of myasthenia gravis models .
|
-
- HY-P990107
-
|
TGF-β Receptor
|
Cancer
|
Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
|
-
- HY-P990117
-
|
Integrin
|
Cardiovascular Disease
Cancer
|
Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
|
-
- HY-P990148
-
|
VEGFR
|
Cancer
|
Anti-Mouse VEGF-A Antibody (2G11-2A05) is a rat-derived IgG2a κ type antibody inhibitor, tragrting to mouse VEGF-A with high affinity. Anti-Mouse VEGF-A Antibody (2G11-2A05) shows good anti-tumor effect in gastric cancer xenograft models .
|
-
- HY-P990257
-
|
c-Fms
|
Cancer
|
Anti-Mouse CSF1 Antibody (5A1) is a rat-derived anti-mouse CSF1 IgG1 κ type antibody inhibitor. Anti-Mouse CSF1 Antibody (5A1) can inhibit cells proliferation and macrophage-induced invasion. Anti-Mouse CSF1 Antibody (5A1) shows potent anti-tumor effect in various tumor models, such as neuroblastoma .
|
-
- HY-P990264
-
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
Anti-Mouse CD70 Antibody (FR70) is a rat-derived ant-mouse CD70 IgG2b κ type antibody inhibitor. Anti-Mouse CD70 Antibody (FR70) decreases CD4 +, CD8 + T cells and eosinophils. Anti-Mouse CD70 Antibody (FR70) shows potent anti-inflammatory and anti-immune effects on allergic lung inflammation and cardiac transplant mice models .
|
-
- HY-P99171
-
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
- HY-P99124
-
|
CD3
|
Inflammation/Immunology
|
Anti-Mouse CD3 Antibody (17A2) is an anti-mouse CD3 IgG2b antibody inhibitor derived from the host Rat. Anti-Mouse CD3 Antibody (17A2) enhances T-cell proliferation and activation and stimulate IFN-γ or IL-17 production in splenic T cells. Anti-Mouse CD3 Antibody (17A2) significantly suppresses mortality in Graft-versus-host disease (GVHD) mice models .
|
-
- HY-P990259
-
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
- HY-P991358
-
LFA-102; X213
|
Estrogen Receptor/ERR
|
Cancer
|
XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting PRLR/Prolactin Receptor. XOMA-213 inhibits hPRL-dependent growth of BaF3/hPRLR cells (EC50: 0.5 μg/mL). XOMA-213 inhibits PRLR signaling and tumor growth in the Nb2-11-luc xenograft mouse model and the DMBA-induced rat breast cancer model. XOMA-213 can be used in Breast cancer, Hyperprolactinaemia and Prostate cancer research .
|
-
- HY-P990792
-
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
Anti-Mouse CD4 Antibody (GK1.5) is an anti-mouse CD4 IgG2b monoclonal antibody. Anti-Mouse CD4 Antibody (GK1.5) can significantly deplete CD4 + T cells. Anti-Mouse CD4 Antibody (GK1.5) can extend the survival rate of xenograft models. Anti-Mouse CD4 Antibody (GK1.5) can be used for research on immunology. The recommend isotype control of Anti-Mouse CD4 Antibody (GK1.5): Rat IgG2b kappa, Isotype Control (HY-P990682) .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N3710
-
-
-
- HY-119580
-
-
-
- HY-N2493
-
-
-
- HY-N9737
-
-
-
- HY-119580R
-
-
-
- HY-N2493R
-
-
-
- HY-N14177
-
-
-
- HY-N14176
-
-
-
- HY-138063
-
-
-
- HY-N8249
-
-
-
- HY-W587784
-
-
-
- HY-N0265
-
-
-
- HY-113427
-
-
-
- HY-N0665
-
-
-
- HY-N2995
-
-
-
- HY-N0321
-
-
-
- HY-W015815
-
-
-
- HY-119821R
-
|
Structural Classification
Microorganisms
Source classification
Phenols
Polyphenols
|
Reference Standards
Glycosidase
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
-
- HY-N0665R
-
-
-
- HY-Y0546
-
|
Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
|
Endogenous Metabolite
Photosensitizer
|
Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
-
- HY-113427R
-
-
-
- HY-W015815R
-
|
Alkaloids
Source classification
Pyridine Alkaloids
Endogenous metabolite
|
Endogenous Metabolite
|
6-Methylnicotinamide is a nicotinamide derivative. 6-methylnicotinamide is also an endogenous metabolite and its sudden increase in the acute stages of intracerebral hemorrhage (ICH) exacerbates neurological damages in rat model. 6-Methylnicotinamide can significantly enhance the coordination effect between acylamino and undercoordinated defective Pb2+ cations. 6-Methylnicotinamide results in enhanced efficiency of perovskite solar cells to 24.33% with excellent environmental storage, heat, and light stabilities .
|
-
-
- HY-B1350A
-
-
-
- HY-N2840
-
-
-
- HY-N0194
-
-
-
- HY-Y0546R
-
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Reference Standards
Endogenous Metabolite
Photosensitizer
|
Benzophenone (Standard) is the analytical standard of Benzophenone. This product is intended for research and analytical applications. Benzophenone standard is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone standard can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone standard can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone standard exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone standard exhibits estrogenic activity .
|
-
-
- HY-N4107
-
-
-
- HY-N4107R
-
-
-
- HY-N0194R
-
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Tagetes lucida Cav.
Umbelliferae
Plants
|
Reference Standards
Apoptosis
Parasite
|
Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
-
- HY-N2840R
-
Allodulcitol (Standard)
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Reference Standards
Drug Intermediate
Bacterial
|
D-Tartaric acid (Standard) is the analytical standard of D-Tartaric acid. This product is intended for research and analytical applications. Allitol is a rare natural polyol that can be used as a sweetener. Allitol is a sugar alcohol formed by linking D- and L-hexoses in a process called izumoring. Allitol has anti-diabetic effects in a long-term allitol diet rat model. Allitol significantly increases the phylum Bacillota and decreases the phyla Bacteroidetes Actinomycetota, and Pseudomonadota. Allitol significantly increases the levels of butyric acid-metabolizing enzymes in a PICRUSt2 gut microbiota analysis. Allitol is an important intermediate for the preparation of the agents which against diabetes, cancer, and viral infections, including AIDS .
|
-
-
- HY-N3847
-
-
-
- HY-N15378
-
|
Structural Classification
Natural Products
Source classification
Spondias mombin L.
Plants
Anacardiaceae
|
IAP
Bcl-2 Family
COX
TNF Receptor
Caspase
Apoptosis
|
β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-Y0546S1
-
|
Benzophenone-d5 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
-
- HY-Y0546S
-
|
Benzophenone-d10 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
-
- HY-W653962
-
|
Triclosan- 13C6 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
-
- HY-B0712S1
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Ceftriaxone- 13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
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- HY-13762S
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Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
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- HY-W747879
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Diclofenac Amide- 13C6 is the 13C-labeled Diclofenac amide (HY-134521). Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
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- HY-B0130S1
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Perindopril-d5 (S-9490-d5) is deuterium labeled Perindopril. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension .
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- HY-113427S
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trans-Vaccenic acid-d13 is deuterium labeled trans-Vaccenic acid (HY-113427). trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
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- HY-169332
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Piezo1 agonist 1-d2 (Compound 12a) is an agonist for Piezo1 with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates the Ca 2+-related ERK signaling pathway, and thus promotes the osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs). Piezo1 agonist 1-d2 ameliorates disuse osteoporosis in the hindlimb-unloading (HU) rat model .
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- HY-Y0546S2
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Benzophenone- 13C is the 13C labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
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- HY-W747491
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Triclosan- 13C12 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
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- HY-134160S
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5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
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- HY-W013403S
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2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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- HY-132610A
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ALN-AS1 sodium
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siRNAs
siRNA drugs
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Givosiran (ALN-AS1) sodium is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran sodium downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran sodium demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran sodium can be used for the research of acute hepatic porphyria (AHP) .
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- HY-132610
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ALN-AS1
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siRNAs
siRNA drugs
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Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran can be used for the research of acute hepatic porphyria (AHP) .
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