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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
31 Results for "
GPCR antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (31)
31 Results for "GPCR antagonist" in MCE Product Catalog:
39
39 Publications Verification
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SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5 .
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2 Cited Publications
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Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs .
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2 Cited Publications
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SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
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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
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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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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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 .
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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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2-Bromo-LSD (BOL-148) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD lacks 5-HT2B agonist activity. 2-Bromo-LSD induces dendritogenesis and spinogenesis. 2-Bromo-LSD reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
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-P4776
CAS No.: 202463-00-1
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CID1231538, a benzothiazole analog, is a potent GPR35 antagonist with no significant activity against rodent orthologs of GPR35, which is also a G protein-coupled receptor (GPCR) .
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Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
Cat. No.: HY-107625
CAS No.: 487051-12-7
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SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
Cat. No.: HY-187528
GPCR antagonist-2 is a GPCR antagonist with macrofilaricidal activity. GPCR antagonist-2 shows inhibitory effects on Brugia pahangi adult females and males (IC50 = 3.9 μM and 2.8 μM, respectively) and Onchocerca ochengi adult females and males (IC50 = 0.35 μM and 1.7 μM, respectively). GPCR antagonist-2 reduces B. pahangi worm burden and affects female fecundity and embryogenesis, downregulates GPCR expression in surviving adult female worms and can be used for the study of filarial infections, including onchocerciasis (river blindness) .
Cat. No.: HY-187424
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GPCR antagonist-1 is an orally active G protein-coupled receptor (GPCR) antagonist as well as an insecticide. GPCR antagonist-1 induces intestinal microvillus destruction, reduces microfilarial secretion, increases the proportion of malformed embryos, inhibits nematode motility and L3-stage molting, and exerts L4-stage larvicidal activity. GPCR antagonist-1 can be used for the research of filarial infections .
Cat. No.: HY-126748
CAS No.: 2223023-78-5
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VUF14862 is a stable and fatigue-resistant photoswitchable GPCR antagonist targeting the histamine H3 receptor (H3R) pathway. VUF14862 binds to H3R with >10-fold increased affinity upon 360 nm irradiation. VUF14862 can be used for spatiotemporal studies of H3R signaling .
Cat. No.: HY-12752BS
CAS No.: 1352792-16-5
Synonyms: Trimeprazine-d6 hydrochloride
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Chlorphenoxamine (Standard) is the analytical standard of Chlorphenoxamine (HY-B1607). This product is intended for research and analytical applications. 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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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
