Search Result
Results for "
transfected
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-16039
-
AM095
Maximum Cited Publications
10 Publications Verification
|
LPL Receptor
|
Inflammation/Immunology
|
|
AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
|
-
-
- HY-122716
-
|
|
PPAR
|
Others
|
|
PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells .
|
-
-
- HY-156460
-
|
|
CCR
|
Inflammation/Immunology
|
|
CMKLR1 antagonist 1 (compound S-26d) is a potent and orally active chemokine-like receptor 1 (CMKLR1) antagonist, with a pIC50 value of 7.44 in hCMKLR1-transfected CHO cells. CMKLR1 antagonist 1 can be used for psoriasis and metabolic diseases research .
|
-
-
- HY-136895
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM) .
|
-
-
- HY-120349
-
|
|
p38 MAPK
JNK
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
LL-Z1640-4 is a potent p38/JNK signaling inhibitor. LL-Z1640-4 significantly diminishes p38 and JNK activation in HCC cells transfected with MLK4 siRNA. LL-Z1640-4 markedly attenuates ROS production induced by MLK4 knockdown. LL-Z1640-4 significantly reduces the apoptotic cells in HCC cells transfected with siMLK4 .
|
-
-
- HY-18941
-
|
LY354740; Eglumetad
|
mGluR
|
Neurological Disease
|
|
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 nM and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.
|
-
-
- HY-P991430
-
|
TB-403
|
VEGFR
|
Cancer
|
|
RO5323441 (TB-403) is a human IgG1 monoclonal antibody (mAb) targeting PLGF. RO5323441 inhibits the binding of human PlGF-1 or PlGF-2 to VEGFR-1 (IC50 values are 0.1 and 0.2 nM, respectively). RO5323441 blocks PlGF-induced VEGFR-1 phosphorylation in Flt-1-transfected HEK293 cells. RO5323441 has antitumor activity .
|
-
-
- HY-130358
-
|
|
Calcium Channel
|
Neurological Disease
|
|
PDDHV is a calcium absorption inducer and may achieve 45Ca 2+ influx by stimulating vanillic acid receptor VR1. PDDHV induces 45Ca 2+ uptake (EC50: 70 nM) in rat dorsal root ganglion neurons (expressing native vanilloid receptors) and calcium mobilization (EC50: 125 nM) in VR1-transfected CHO cells. PDDHV also inhibits [3H]-resiniferatoxin (RTX) binding to the dorsal root ganglion membrane in rats .
|
-
-
- HY-169301
-
|
|
GPR35
|
Cancer
|
|
Gpr35 modulator 1 (compound 1-18) is a potent modulator of Gpr35, with the IC50 of ≤ 100 nM in HEK293 cells stably transfected with human GPR35 .
|
-
-
- HY-157503
-
|
|
Photosensitizer
|
Cancer
|
|
Photosensitizer-3 is a photosensitizer that exhibits powerful selective killing effects on transfected HEK cells and affibody-targeted A431 cancer cells when exposed to near-infrared light excitation .
|
-
-
- HY-110003
-
|
ACPA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM) .
|
-
-
- HY-133551
-
|
|
RET
|
Cancer
|
|
WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration .
|
-
-
- HY-19408
-
Pyr10
3 Publications Verification
|
TRP Channel
|
Others
|
|
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels .
|
-
-
- HY-156696
-
|
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
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 .
|
-
-
- HY-163739
-
|
|
α-synuclein
|
Neurological Disease
|
|
LETC is an orally active α-synuclein (α-Syn) aggregation inhibitor with an EC50 of 66 nM in transfected DH60.21 neuroblastoma cells. LETC can cross the blood-brain barrier. LETC can be used for the study of synucleinopathies .
|
-
-
- HY-169603
-
|
|
FAAH
|
Metabolic Disease
|
|
AZ513 is a reversible FAAH inhibitor with an IC50s of 551 nM and 27 nM for human FAAH and rat FAAH, respectively. AZ513 inhibits Anandamide (HY-10863) hydrolysis in human FAAH-transfected HEK293 cells (IC50 of 360 nM) .
|
-
-
- HY-N15419
-
|
|
HBV
|
Infection
|
|
Acutumidine (compound 4) is an alkaloid with anti-HBV activity that can be isolated from Hypserpa nitida Miers. Acutumidine inhibits the production of HBsAg in Hep G2.2.15 cells stably transfected with HBV genome with an IC50 value of 2.023 mM .
|
-
-
- HY-W754691
-
|
|
HBV
|
Infection
|
|
Glaziovine is an antiviral agent found in Hypserpa nitida. Glaziovine exhibits significant inhibitory activity against HBV, capable of suppressing hepatitis B virus surface antigen (HBsAg) secretion in Hep G2.2.15 cells transfected with HBV, with an IC50 of 8 nM .
|
-
-
- HY-100678
-
|
|
Adenosine Receptor
PI3K
|
Inflammation/Immunology
Cancer
|
|
CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .
|
-
-
- HY-160225
-
|
|
STING
|
Inflammation/Immunology
|
|
ISD (interferon stimulatory DNA) sodium is a non-CpG oligomer from the Listeria monocytogenes genome. When transfected into cells, ISD sodium strongly enhances the expression of IFN-β. This ISD-induced response is mediated by the STING-TBK1-IRF3 signaling axis .
|
-
-
- HY-168371
-
|
|
Scavenger Receptor Class B type I (SR-BI）
|
Metabolic Disease
|
|
1-Palmitoyl-2-13(S)-HODE-sn-glycero-3-PC (13-HODE-PC) is an oxidized phospholipid that contains Palmitic acid (HY-N0830) and 13(S)-HODE (HY-113884B) at the sn-1 and sn-2 positions, respectively. 1-Palmitoyl-2-13(S)-HODE-sn-glycero-3-PC has the ability to compete for the binding of 125I-NO2-LDL (5 g/mL) to CD36-transfected 293 cells, with the IC50 of ＞ 200 μM .
|
-
-
- HY-18941B
-
|
(rel)-LY354740; (rel)-Eglumetad
|
mGluR
|
Neurological Disease
|
|
(rel)-Eglumegad ((rel)-LY354740) is a relative configuration of Eglumegad (HY-18941). Eglumegad is a highly potent and selective group II (mGlu2/3) receptor agonist with EC50s of 5 and 24 nM for transfected human mGlu2 and mGlu3 receptors, respectively .
|
-
-
- HY-P3789
-
|
|
Orphan Receptor
|
Metabolic Disease
|
|
Prolactin-Releasing Peptide (12-31), rat is a fragment of the prolactin releasing peptide (PrRP). Prolactin-Releasing Peptide (12-31), rat shows high affinity for GPR10 receptors. Prolactin-Releasing Peptide (12-31), stimulates calcium mobilization in CHOK1 cells transfected with the PrRP receptor .
|
-
-
- HY-115292
-
|
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Simvastatin hydroxy acid (Tenivastatin) sodium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin hydroxy acid sodium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin hydroxy acid sodium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
|
-
-
- HY-119695B
-
|
Tenivastatin calcium hydrate
|
HMG-CoA Reductase (HMGCR)
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Simvastatin acid (Tenivastatin) calcium hydrate is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid calcium hydrate reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid calcium hydrate can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
|
-
-
- HY-18941C
-
|
LY354740 hydrochloride; Eglumetad hydrochloride
|
mGluR
|
Neurological Disease
|
|
Eglumegad (LY354740) hydrochloride is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively. Eglumegad hydrochloride protects neurons from NMDA toxicity. Eglumegad hydrochloride has anxiolytic- and antipsychotic-like effects .
|
-
-
- HY-119695A
-
-
-
- HY-142922
-
|
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11) .
|
-
-
- HY-162837
-
|
|
Aurora Kinase
|
Cancer
|
|
AURKA against 1 is an inhibitor of AURKA (IC50 less than 0.5 nM), targeting endogenous lysine (K162) acetylation, and has anti-proliferation activity against tumor cells. AURKA against 1 induces K162 acetylation, and the kinase activity of AURKA is reversibly restored in HCT116 cells transfected with SIRT3 .
|
-
-
- HY-119695
-
-
-
- HY-139052
-
|
|
γ-secretase
|
Neurological Disease
|
|
III-31-C is a (hydroxyethyl)urea γ-secretase inhibitor. III-31-C inhibits Aऔ production with an IC50 of 10 nM in the cell-free γ-secretase assay and 200 nM in APP-transfected cells. III-31-C can be used in Alzheimer's disease research .
|
-
-
- HY-112378
-
|
|
FLT3
|
Cancer
|
|
D-65476 is an inhibitor of type Ⅲ receptor tyrosine kinase (Flt3). In the absence of IL-3, D-65476 inhibits the proliferation of TEL-Flt3 transfected BA/F3 cells (IC50= 0.2 μM), which can be used in the study of Flt3-driven leukemia .
|
-
-
- HY-117999
-
|
|
HBV
|
Infection
|
|
BAY39-5493 is a non-nucleoside inhibitor that inhibits HBV replication. BAY39-5493 inhibits viral DNA replication by preventing the formation of viral core particles (nucleocapsids). The IC50 value of BAY39-5493 against HBV in stably transfected HepG2.2.15 cells is 0.03 μM .
|
-
-
- HY-116607
-
|
|
HBV
|
Infection
|
|
BAY38-7690 is a non-nucleoside inhibitor that inhibits HBV replication. BAY38-7690 inhibits viral DNA replication by preventing the formation of viral core particles (nucleocapsids). The IC50 value of BAY38-7690 against HBV in stably transfected HepG2.2.15 cells is 0.15 μM .
|
-
-
- HY-100678R
-
|
|
Reference Standards
Adenosine Receptor
PI3K
|
Inflammation/Immunology
Cancer
|
|
CGS 15943 (Standard) is the analytical standard of CGS 15943. This product is intended for research and analytical applications. CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .
|
-
-
- HY-B0528
-
|
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
|
Octopamine is a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
|
-
-
- HY-103118
-
|
|
5-HT Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively .
|
-
-
- HY-114141
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
|
BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively . BI-671800 has potential for the treatment of poorly controlled asthma .
|
-
-
- HY-B0528A
-
|
(±)-p-Octopamine hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
|
Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
|
-
-
- HY-101189B
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
|
-
-
- HY-101189
-
|
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
|
-
-
- HY-P1318
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
-
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
-
- HY-119695AR
-
|
Tenivastatin ammonium (Standard)
|
Reference Standards
HMG-CoA Reductase (HMGCR)
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Simvastatin acid (ammonium) (Standard) is the analytical standard of Simvastatin acid (ammonium). This product is intended for research and analytical applications. Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
|
-
-
- HY-119695AS1
-
-
-
- HY-119695S
-
-
-
- HY-119695AS
-
|
Tenivastatin-d6 ammonium
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
|
-
-
- HY-103565
-
AMN082
1 Publications Verification
|
mGluR
|
Neurological Disease
|
|
AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
-
- HY-B0528AS
-
|
(±)-p-Octopamine-d4 hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
|
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
|
-
-
- HY-143218
-
|
Tetraphenylethene maleimide
|
Huntingtin
Parasite
|
Infection
Neurological Disease
|
|
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells (the excitation wavelength is 350 nm and the emission wavelength is 470 nm). TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
|
-
- HY-P5894
-
|
Galanin-like peptide (3-32)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
|
-
- HY-B0920
-
|
U-17835
|
Potassium Channel
|
Metabolic Disease
Endocrinology
|
|
Tolazamide (U-17835) is an orally active sulfonylurea agent that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (IC50 = 4.2 µM in HEK293 cells transfected with the human receptor). Tolazamide has anti-diabetic properties. Tolazamide can lower blood glucose in sulfonylurea class. Tolazamide decreases insulin dose while continuing to maintain adequate metabolic control. Tolazamide is able to improve or normalize hyperglycemia and HbA .
|
-
- HY-125102
-
|
|
IGF-1R
|
Cancer
|
|
AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
|
-
- HY-B0528AR
-
|
(±)-p-Octopamine hydrochloride (Standard)
|
Reference Standards
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
|
Octopamine (hydrochloride) (Standard) is the analytical standard of Octopamine (hydrochloride). This product is intended for research and analytical applications. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
|
-
- HY-103565A
-
|
|
mGluR
|
Neurological Disease
|
|
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-126862
-
|
|
mAChR
|
Others
|
|
AQ-RA 721 is a muscarinic receptor antagonist with differential affinity for the m4 and M2 sites, which can be used to characterize muscarinic receptor subtypes. Other muscarinic receptor antagonists have differential affinity for the M1 (rat cerebral cortex), M2 (rat heart), M3 (rat submandibular gland), m4 (receptor expressed in Chinese hamster ovary cells transfected with CHO), and guinea pig uterine smooth muscle at the muscarinic binding site .
|
-
- HY-19858
-
|
|
iGluR
|
Neurological Disease
|
|
LY-466195 is a selective and competitive GLUK5 receptor antagonist. LY-466195 antagonizes Kainate-induced currents with an IC50 value of 0.045 μM in rat dorsal root ganglion neurons. In HEK293 cells transfected with GLUK5, GLUK2/GLUK5, or GLUK5/GLUK66 receptors, LY466195 produces IC50 values of 0.08 μM, 0.34 μM, and 0.07 μM, respectively .
|
-
- HY-103565R
-
|
|
Reference Standards
mGluR
|
Neurological Disease
|
|
AMN082 (Standard) is the analytical standard of AMN082. This product is intended for research and analytical applications. AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-164474
-
|
|
MEK
|
Cancer
|
|
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
|
-
- HY-160222
-
|
|
HSV
STING
|
Infection
Inflammation/Immunology
|
|
HSV-60mer sodium is a 60 bp double-stranded oligonucleotide containing viral DNA motifs that derive from the herpes simplex virus 1 (HSV-1) genome . Transfected HSV-60 has been shown to potently induce IFN-β in a Toll-like receptor (TLR)-, DNA-dependent activator of IRFs (DAI)-, and RNA polymerase III (Pol III)-independent, but STING-, TBK1- and IFN regulatory factor 3 (IRF3)-dependent manner.
|
-
- HY-B0920R
-
|
U-17835 (Standard)
|
Reference Standards
Potassium Channel
|
Metabolic Disease
Endocrinology
|
|
Tolazamide (U-17835) (Standard) is the analytical standard of Tolazamide. This product is intended for research and analytical applications. Tolazamide is an orally active sulfonylurea agent that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (IC50 = 4.2 µM in HEK293 cells transfected with the human receptor). Tolazamide has anti-diabetic properties. Tolazamide can lower blood glucose in sulfonylurea class. Tolazamide decreases insulin dose while continuing to maintain adequate metabolic control. Tolazamide is able to improve or normalize hyperglycemia and HbA .
|
-
- HY-135783
-
AT 1001
1 Publications Verification
|
nAChR
|
Neurological Disease
|
|
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
|
-
- 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-121579
-
|
|
PPAR
|
Others
|
|
L-764406 is a non-thiazolidinedione (TZD)-type PPARg nuclear receptor ligand with high affinity. L-764406 has significant binding ability to PPARg (IC50=70 nM). L-764406 exhibited partial agonist activity and induced expression of the adipocyte-specific gene aP2 in chimeric receptors expressing the PPARg LBD and the corresponding reporter gene, as well as in 3T3-L1 cells. In contrast, L-764406 showed no activity in cells transfected with chimeric receptors containing PPARa or PPARd LBDs .
|
-
- HY-103565AR
-
|
|
Reference Standards
mGluR
|
Neurological Disease
|
|
AMN082 (free base) (Standard) is the analytical standard of AMN082 (free base). This product is intended for research and analytical applications. AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-W011121
-
|
2-OG
|
GPR119
NF-κB
TGF-beta/Smad
GLP Receptor
|
Metabolic Disease
|
|
2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
|
-
- HY-155141
-
|
|
Cytochrome P450
|
Cancer
|
|
hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM) .
|
-
- HY-156584
-
|
|
Endogenous Metabolite
|
Infection
|
|
ODE-Bn-PMEG is an antiviral compound with strong inhibitory activity against HPV-11, -16, and -18. ODE-Bn-PMEG effectively reduced transient amplification of viral DNA in transfected cells at concentrations well below its cytotoxic levels. ODE-Bn-PMEG showed increased uptake in human foreskin fibroblasts and was able to be efficiently converted to the active antiviral metabolite PMEG diphosphate in vitro. The P-chiral enantiomer of ODE-Bn-PMEG showed comparable antiviral activity, indicating its potential application against multiple HPV types. ODE-Bn-PMEG is a promising candidate for local inhibition of HPV-16, HPV-18, and other high-risk types .
|
-
- HY-156086
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA G595R, TRKA G667C and TRKA F589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM .
|
-
- HY-174215
-
|
|
Tau Protein
|
Neurological Disease
|
|
TAU-IN-3 (Compound 2) is an orally active TAU inhibitor. TAU-IN-3 inhibits the expression of MAPT exon 10 DDPAC mutant gene in HeLa cells (IC50: 0.6 µM). TAU-IN-3 reduces the 4R/3R MAPT mRNA ratio in HeLa cells transfected with WT or DDPAC minigenes. TAU-IN-3 inhibits the insertion of endogenous MAPT exon 10 and the production of 4R tau protein in cells. TAU-IN-3 modulates tau splicing in htau mice and improves the associated behavioral phenotypes. TAU-IN-3 can be used to study neurodegenerative diseases .
|
-
- HY-173033
-
|
|
Constitutive Androstane Receptor
Cytochrome P450
|
Metabolic Disease
|
|
MI-883 is the orally active agonist for Constitutive Androstane Receptor (CAR, EC50=73 nM) and the antagonist for Pregnane X Receptor (PXR, IC50=0.1 μM). MI-883 stimulates CAR LBD assembly (EC50=0.38 µM) and CAR3 variant activation (EC50=0.074 µM), induces CYP2B6 mRNA expression in HepaRG and primary human hepatocytes. MI-883 inhibits basal PXR activity IC50=2.03 µM) in transiently transfected HepG2 cells, blocks CYP3A4 mRNA expression in HepG2. MI-883 regulates cholesterol metabolism and bile acid excretion, improves hypercholesterolemia in mouse models .
|
-
- HY-W701772
-
|
2-OG-d5
|
Isotope-Labeled Compounds
GPR119
TGF-beta/Smad
NF-κB
GLP Receptor
|
Metabolic Disease
|
|
2-Oleoylglycerol-d5 (2-OG-d5) is the deuterium labeled 2-Oleoylglycerol (HY-W011121). 2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
|
-
- HY-149359
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
|
-
- HY-N0322B
-
|
|
Liposome
Endogenous Metabolite
|
Others
|
Cholesterol (Excipient, GMP Like) is the GMP Like class Cholesterol (HY-N0322), and can be used as pharmaceutical excipients. Cholesterol is a component of the cell membrane and a precursor of some hormones, vitamin D and bile acid, with oral activity.
In Vitro: Cholesterol (200 μg/mL; 40 h) increases the production of newly synthesized β-amyloid protein and enhances the secretion of Aβ1-40 in HEK cells transfected with APP .
In Vivo: Cholesterol (0.5% cholesterol in diet; oral; once daily; 7 days) increases plasma cholesterol in the hamster model, while the cholesterol absorption inhibitor SCH 48461 (10 mg/kg; oral gavage; once daily; 7 days) inhibits cholesterol absorption and reduces plasma cholesterol .
Cholesterol (1% cholesterol + 0.5% bile acid in diet; oral; once daily; 7 days) increases plasma cholesterol levels in the male CD rat model, while SCH 48461 (2 mg/kg; oral; once daily; 7 days) reduces hepatic cholesterol ester accumulation .
Cholesterol (0.25% cholesterol + 22% saturated fat diet; oral; once daily; 3 weeks) increases VLDL+LDL cholesterol levels in the rhesus monkey model, while SCH 48461 (0.2 mg/kg; oral; once daily; 3 weeks) maintains baseline levels and inhibits cholesterol absorption .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-143218
-
|
Tetraphenylethene maleimide
|
Fluorescent Dyes/Probes
|
|
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells (the excitation wavelength is 350 nm and the emission wavelength is 470 nm). TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3789
-
|
|
Orphan Receptor
|
Metabolic Disease
|
|
Prolactin-Releasing Peptide (12-31), rat is a fragment of the prolactin releasing peptide (PrRP). Prolactin-Releasing Peptide (12-31), rat shows high affinity for GPR10 receptors. Prolactin-Releasing Peptide (12-31), stimulates calcium mobilization in CHOK1 cells transfected with the PrRP receptor .
|
-
- HY-P10477
-
|
|
Peptides
|
Cancer
|
|
CT-08 (CT8, Compound 3) is a macrocyclic Sec61 modulator, blocks protein secretion in a signal sequence-dependent manner. CT-08 blocks Sec61-mediated translocation of VCAMss-GLuc into the ER, resulting in a loss of luciferase activity. CT-08 inhibits VCAM expression in transfected cells .
|
-
- HY-P1318
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P5894
-
|
Galanin-like peptide (3-32)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with high affinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P991430
-
|
TB-403
|
VEGFR
|
Cancer
|
|
RO5323441 (TB-403) is a human IgG1 monoclonal antibody (mAb) targeting PLGF. RO5323441 inhibits the binding of human PlGF-1 or PlGF-2 to VEGFR-1 (IC50 values are 0.1 and 0.2 nM, respectively). RO5323441 blocks PlGF-induced VEGFR-1 phosphorylation in Flt-1-transfected HEK293 cells. RO5323441 has antitumor activity .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0528AS
-
|
|
|
Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure .
|
-
-
- HY-119695AS1
-
|
|
|
Simvastatin acid-d9 ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
|
-
-
- HY-119695S
-
|
|
|
Simvastatin acid-d6 (Tenivastatin-d6) is deuterium labeled Simvastatin acid. Simvastatin acid (Tenivastatin), a hydrolysate of Simvastatin (HY-17502), is a HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
|
-
-
- HY-119695AS
-
|
|
|
Simvastatin acid-d6 (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
|
-
-
- HY-W701772
-
|
|
|
2-Oleoylglycerol-d5 (2-OG-d5) is the deuterium labeled 2-Oleoylglycerol (HY-W011121). 2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-160225
-
|
|
|
CpG ODNs
|
|
ISD (interferon stimulatory DNA) sodium is a non-CpG oligomer from the Listeria monocytogenes genome. When transfected into cells, ISD sodium strongly enhances the expression of IFN-β. This ISD-induced response is mediated by the STING-TBK1-IRF3 signaling axis .
|
-
- HY-N0322B
-
|
|
|
Emulsifiers
Liposomal Film-forming Agents
|
Cholesterol (Excipient, GMP Like) is the GMP Like class Cholesterol (HY-N0322), and can be used as pharmaceutical excipients. Cholesterol is a component of the cell membrane and a precursor of some hormones, vitamin D and bile acid, with oral activity.
In Vitro: Cholesterol (200 μg/mL; 40 h) increases the production of newly synthesized β-amyloid protein and enhances the secretion of Aβ1-40 in HEK cells transfected with APP .
In Vivo: Cholesterol (0.5% cholesterol in diet; oral; once daily; 7 days) increases plasma cholesterol in the hamster model, while the cholesterol absorption inhibitor SCH 48461 (10 mg/kg; oral gavage; once daily; 7 days) inhibits cholesterol absorption and reduces plasma cholesterol .
Cholesterol (1% cholesterol + 0.5% bile acid in diet; oral; once daily; 7 days) increases plasma cholesterol levels in the male CD rat model, while SCH 48461 (2 mg/kg; oral; once daily; 7 days) reduces hepatic cholesterol ester accumulation .
Cholesterol (0.25% cholesterol + 22% saturated fat diet; oral; once daily; 3 weeks) increases VLDL+LDL cholesterol levels in the rhesus monkey model, while SCH 48461 (0.2 mg/kg; oral; once daily; 3 weeks) maintains baseline levels and inhibits cholesterol absorption .
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
