Search Result
Results for "
SD rats
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-110116
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MMP
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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SD-2590 hydrochloride is a potent MMP inhibitor with IC50 values of ﹤0.1, ﹤0.1, 0.18, and 1.7 nM for MMP2, MMP13, MMP9, and MMP8, respectively. SD-2590 hydrochloride inhibits dilation of the left ventricle in rats .
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- HY-D2868
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DAPI
Maximum Cited Publications
90 Publications Verification
4',6-Diamidino-2-phenylindole
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Sodium Channel
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Neurological Disease
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DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment .
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- HY-105090
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats .
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- HY-163536
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TGF-beta/Smad
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Inflammation/Immunology
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TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency .
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- HY-161505
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Transthyretin (TTR)
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Others
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Transthyretin-IN-3 (compound 6) is a designed benzofuran analogue. Transthyretin-IN-3 selectively binds to plasma transthyretin (TTR) to inhibit Amyloid aggregation (IC50=5.0±0.2 μM). Transthyretin-IN-3 can bind to TTR's thyroxine binding site specifically by carrying chlorine substituents at specific locations in its structure. This binding can prevent TTR tetramers from dissociating into unstable monomers .
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- HY-174383
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE3/4-IN-2 (Compound 1) is a PDE3/PDE4 dual-target inhibitor, with IC50 values of 0.13 nM and 50 nM against PDE3A and PDE4B1, respectively. PDE3/4-IN-2 can be used in the research of PDE-related diseases, such as asthma, obstructive pulmonary disease, sepsis, and nephritis .
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- HY-167654
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Others
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Cardiovascular Disease
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Treloxinate is an effective hypolipidemic agent. Treloxinate affects only triglyceride levels in Sprague-Dawley rats, but affects both triglyceride and cholesterol levels in Wistar rats .
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- HY-105090R
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Reference Standards
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
Cancer
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Lerisetron (Standard) is the analytical standard of Lerisetron. This product is intended for research and analytical applications. Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats .
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- HY-168713
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FXR
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Metabolic Disease
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LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
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- HY-106816
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- HY-18211
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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CGS 35601 is the inhibitor for endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), with IC50s of 55, 2, and 22 nM, respectively. CGS 35601 suppresses the big endothelin-1 (big ET-1)- and angiotensin I-induced pressor response, and enhances circulation of atrial natriuretic peptide (ANP), regulates the cardiovascular function in SD rats .
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- HY-P10318
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GLP Receptor
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Endocrinology
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SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
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- HY-174260
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NO Synthase
COX
Caspase
MDM-2/p53
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Neurological Disease
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Neuroprotective agent 11 (Compound 1a) is an orally active polyphenol compound with significant protective effects against cerebral ischemia. The main activities of Neuroprotective agent 11 include inhibiting neuronal inflammation and apoptosis, reducing cerebral infarction volume, and improving behavioral symptoms of cerebral ischemic mice. Neuroprotective agent 11 exerts its regulatory mechanism by downregulating the expression of inflammatory factors (iNOS、COX-2) and apoptotic proteins (cleaved-Caspase3, p53). Neuroprotective agent 11 can be used in the study of cerebral ischemia-related diseases (such as ischemic stroke) .
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- HY-144801
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Potassium Channel
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Cardiovascular Disease
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DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine .
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- HY-144801A
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Potassium Channel
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Cardiovascular Disease
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DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine .
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- HY-162438
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HIF/HIF Prolyl-Hydroxylase
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Metabolic Disease
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PHD2-IN-2 (Compound 12) is a PHD2 inhibitor, with an IC50 of 34.3 nM. PHD2-IN-2 has high erythropoietin (EPO) inducing activity, with an EC50 of 6.79 μM. PHD2-IN-2 can be used for the research of anemia, ischemia, and hypoxia .
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- HY-162583
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-17 (compound 4e) is a potent PDE4 inhibitor. PDE4-IN-17 inhibits PDE4B and PDE4D with IC50s of 10.0 and 15.2 nM, respectively. PDE4-IN-17 has good oral bioavailability (F=66%) and longer half-life (t1/2=2.0 h) in SD rats .
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- HY-17610A
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TS-091 hydrochloride
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Histamine Receptor
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Neurological Disease
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Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
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- HY-160888
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mAChR
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Endocrinology
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ASP8302 is a positive and allosteric muscarinic M3 receptor modulator. ASP8302 improves voiding efficiency and reduced residual urine volume in two voiding dysfunction models. ASP8302 can be used for research of underactive bladder .
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- HY-163505
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Bacterial
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Others
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Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
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- HY-176706
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AAK1
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Neurological Disease
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AAK1-IN-10 (Compound 1-2) is an AAK1 inhibitor. AAK1-IN-10 has significant AAK1 enzyme inhibitory activity (IC50: 9.62 nM). AAK1-IN-10 mainly exerts its effects by inhibiting the activity of connexin-associated kinase 1 (AAK1). AAK1-IN-10 has low cardiotoxicity (IC50 = 13.7 μM). AAK1-IN-10 can be used in the study of diabetic neuropathy and postherpetic pain .
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- HY-174126
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P2Y Receptor
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Cardiovascular Disease
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P2Y1 antagonist 2 (Compound 19) is a P2Y1 receptor antagonist (IC50: 0.49 μM). P2Y1 antagonist 2 has significant antiplatelet aggregation activity and exerts its effects by inhibiting P2Y1 receptor. P2Y1 antagonist 2 can upregulate nuclear Nrf2 protein levels, exhibit neuroprotective effects, and resist oxidative stress damage. P2Y1 antagonist 2 can effectively reduce cerebral infarction area and improve neurobehavioral function, and can be used in the study of ischemic stroke .
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- HY-17610
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TS-091
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Histamine Receptor
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Neurological Disease
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Enerisant (TS-091) is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
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- HY-N8903
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- HY-176205
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AB801
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TAM Receptor
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Cancer
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Ligritinib (AB801) is an orally active AXL receptor tyrosine kinase inhibitor. Ligritinib blocks the downstream signaling pathway by inhibiting the kinase activity of AXL. Ligritinib can be used in cancer research, especially in combination with chemotherapy for non-small cell lung cancer (NSCLC) .
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- HY-174428
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JAK
STAT
PROTACs
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Cancer
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PROTAC JAK2 degrader-1 (Compound 10i) is a JAK2 PROTAC degrader with a DC50 of 27.35 nM for JAK2 V617F. PROTAC JAK2 degrader-1 promotes the ubiquitination and degradation of JAK2. PROTAC JAK2 degrader-1 inhibits the phosphorylation of JAK2, STAT3 and STAT5. PROTAC JAK2 degrader-1 can be used in the research of myeloproliferative neoplasms (Pink: JAK2 ligand (HY-174430); Blue: E3 ligase ligand (HY-W087383); Black: E3 ligase ligand + linker (HY-174432)) .
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- HY-150080
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BMS-986180
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HIV
HIV Integrase
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Infection
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GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
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- HY-171033
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Phospholipase
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Neurological Disease
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ASM-IN-3 (Compound 21b) is a selective and BBB-penetrating acid sphingomyelinase (ASM) inhibitor (IC50: 3.37 μM for pure human ASM). ASM-IN-3 improves depression-like behaviors by inhibiting ASM activity and increasing neurogenesis in hippocampus in Reserpine (HY-N0480)-induced depressed rats .
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- HY-152535
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HSV
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Infection
Inflammation/Immunology
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ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
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- HY-163207
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Epoxide Hydrolase
HDAC
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Neurological Disease
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sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC50s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects .
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- HY-143406
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Fungal
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Infection
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Antifungal agent 25 is a potent broad-spectrum antifungal agent. Antifungal agent 25 shows antifungal effect against Candida albicans and fluconazole-resistant strain of Candida albicans. Antifungal agent 25 stable metabolic property in vivo .
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- HY-101481
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COX
Apoptosis
MEK
ERK
PPAR
AMPK
NF-κB
Interleukin Related
TNF Receptor
STAT
Wnt
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Neurological Disease
Inflammation/Immunology
Cancer
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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-115989
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HCV
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Infection
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HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
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- HY-175230
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Lactate Dehydrogenase
Apoptosis
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Cancer
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ZG-2492 is an orally active LDHA inhibitor with an IC50 of 156 nM. ZG-2492 can reduce lactate production and induce cell cycle arrest and apoptosis in pancreatic cancer cells . ZG-2492 has antitumor activity and can be used in the research of tumors such as pancreatic cancer .
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- HY-115986
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Monoamine Oxidase
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Neurological Disease
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MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.204 µM. MAO-B-IN-5 has the potential for the research of Parkinson's disease (PD) .
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- HY-168954
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c-Fms
Apoptosis
Akt
ERK
STAT
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Inflammation/Immunology
Cancer
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CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22% .
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- HY-101481R
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Reference Standards
COX
Apoptosis
MEK
ERK
PPAR
AMPK
NF-κB
Interleukin Related
TNF Receptor
STAT
Wnt
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Neurological Disease
Inflammation/Immunology
Cancer
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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-N0108
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Parietin; Rheochrysidin
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Bacterial
Toll-like Receptor (TLR)
NF-κB
Apoptosis
Autophagy
Antibiotic
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Infection
Inflammation/Immunology
Cancer
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Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells .
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- HY-144658
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Factor Xa
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Cardiovascular Disease
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FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
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- HY-109968A
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CEP-26401 hydrochloride
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Histamine Receptor
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Neurological Disease
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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 .
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- HY-109968
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CEP-26401
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Histamine Receptor
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Neurological Disease
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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 .
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- HY-155489
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Anaplastic lymphoma kinase (ALK)
Apoptosis
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Cancer
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DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4 11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
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- HY-170576
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FLT3
STAT
Apoptosis
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Cancer
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FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .
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Cat. No. |
Product Name |
Type |
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- HY-D2868
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4',6-Diamidino-2-phenylindole
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Fluorescent Dyes/Probes
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DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10318
-
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GLP Receptor
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Endocrinology
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SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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