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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
164 Results for "
GPCR multimer
" in MedChemExpress (MCE) Product Catalog:
Products (164)
164 Results for "GPCR multimer" in MCE Product Catalog:
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1 Cited Publications
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BI 6901 is a potent, selective CCR10 antagonist (pIC50=9.0). BI 6901 shows high selectivity over other GPCRs, including a number of other chemokine receptors. BI 6901 is efficacious in the murine DNFB model of contact hypersensitivity and can be used for inflammation research .
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Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids .
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1 Cited Publications
Cat. No.: HY-19838
CAS No.: 1802326-66-4
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JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139). JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB) .
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Chlorphenoxamine, an antihistamine and anticholinergic agent is a GPCR antagonist. Chlorphenoxamine inhibits multiple lethal viral diseases, such as SARS-CoV, MERS-CoV, EBOV and malaria. Chlorphenoxamine shows anti-filovirus activity against both EBOV and Marburg virus (MARV) with IC50s of 1.1 μM and 6.2 μM, respectively. Chlorphenoxamine is used for allergic conditions, urticaria, viral diseases and Parkinson’s disease .
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1 Cited Publications
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UCSF924, a chemical probe, is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has no off-target effects on more than 320 non-olfactory GPCRs. UCSF924 can be used for research in the field of neuropsychiatric diseases .
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Acifran (AY 25712) is an orally active, full GPR109A and GPR109B agonist and hypolipidemic agent. Acifran reduces Forskolin (HY-15371)-induced cAMP elevation, triggers ERK1/ERK2 phosphorylation, and inhibits lipolysis in adipose tissue through Gi-coupled GPCR activation. Acifran is used for research on atherosclerosis, hyperlipidemia, and type 2 diabetes .
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1 Cited Publications
Synonyms: Ursodeoxycholate-d4; Ursodiol-d4; UDCA-d4
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1 Cited Publications
Synonyms: GPR132 antagonist 1
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NOX-6-18 (GPR132 antagonist 1) is a GPR132 antagonist with an IC50 of 15.17 nM against the human target. NOX-6-18 inhibits GPR132 activation via interaction with non-conserved residues, blocks activities induced by endogenous agonists and 9 (S)-HODE, and exhibits selectivity for other fatty acid-binding GPCRs. NOX-6-18 regulates macrophage reprogramming, alleviates inflammatory responses, downregulates inflammatory markers and signaling pathways, and reduces the degree of hepatic steatosis and hepatic triglyceride levels. NOX-6-18 regulates metabolic homeostasis, reduces weight gain, enhances glucose metabolism, improves glucose tolerance, decreases fasting blood glucose and insulin levels, and partially reverses reductions in energy expenditure and respiratory quotient. NOX-6-18 can be used in the research of type 2 diabetes .
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PF-07054894 is an orally active and potent C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) antagonist that blocks CCR6-mediated chemotaxis with an IC50 value of 5.7 nM in vitro. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease .
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects .
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Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice .
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CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension .
Cat. No.: HY-124803
CAS No.: 1407592-99-7
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GPCR modulator-1 is a negative allosteric modulator of the GLP-1 receptor (GLP-1R). GPCR modulator-1 can be used for the study of type 2 diabetes .
Cat. No.: HY-P1769
CAS No.: 34233-50-6
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Cat. No.: HY-177116
CAS No.: 252280-67-4
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GPR15 antagonist-1 (Compound 5) is a GPR15 antagonist. G protein-coupled receptor 15 (GPR15) is an extensively studied GPCRs involving HIV infection, colonic inflammation, and smoking-related diseases .
Cat. No.: HY-133862
CAS No.: 70375-43-8
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SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 µM .
Cat. No.: HY-W010448
CAS No.: 22884-10-2
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
