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GPCR

GPCR

货号 产品名 CAS号 信息
CSN17794 TUG-770 1402601-82-4 TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.
CSN23913 TUG-1375 2247372-59-2 TUG-1375 is a free fatty acid receptor 2 (FFA2/GPR43) inhibitor with pKi of 6.69.
CSN23156 TC-O 9311 444932-31-4 TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM[1].
CSN21268 SB-568849 395679-53-5 SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.
CSN22483 Fezagepras sodium 1254472-97-3 PBI-4050 acts as an agonist for GPR40 and as an antagonist or inverse agonist for GPR84.
CSN21271 NGD-4715 476322-70-0 NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .
CSN22253 Sodium 2-((R)-4-((3R,5S,7R,8R,9S,10S,12S,13R,14S,17R)-3,7,12-trihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)ethane-1-sulfonate (1:1) 145-42-6 Monosodium taurocholate is an agonist of GPBAR1 and is potential of the treatment of type 2 diabetes and obesity in rats.
CSN20277 ML-290 1482500-76-4 ML290 is a biased allosteric agonist at the relaxin receptor RXFP1 possessing a signalling profile indicative of vasodilator and anti-fibrotic properties.
CSN22976 ML-193 713121-80-3 ML 193 is a selective GPR55 antagonist with IC50 of 221 nM.
CSN18472 MK-0354 851776-28-8 MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
CSN22972 MK-1903 1268882-43-4 MK 1903 is a potent and selective hydroxycarboxylic acid receptor 2 (HCA2, GPR109A) full agonist.
CSN22968 MEDICA16 87272-20-6 MEDICA 16 is a free fatty acid 1 (FFA1/GPR40) receptor agonist.
CSN21282 MCHR1 antagonist 2 863115-70-2 MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.
CSN21217 MCH-1 antagonist 1 1039825-68-7 MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
CSN18041 JNJ-63533054 1802326-66-4 JNJ-63533054 is a selective hGPR139 agonist with EC50 of 16 nM.
CSN18985 INT-777 R-enantiomer 1198786-98-9 INT-777 R-enantiomer is the R-enantiomer of INT-777, with EC50 of 4.79 μM for TGR5, and less potent than INT-777.
CSN23709 GW-803430 515141-51-2 GW 803430 is a selective melanin-concentrating hormone receptor 1 (MCH1) antagonist with IC50 of 9.3 nM.
CSN22421 GPR84 antagonist 8 1445846-30-9 GPR84 antagonist 8 is a selective GPR84 antagonist.
CSN20435 GPR4 antagonist 1 1197879-16-5 GPR4 antagonist C39c shows potent cellular activity and is efficacious in animal models of angiogenesis, inflammation and pain.
CSN22236 GPR120 Agonist 2 1234844-11-1 GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
CSN20374 GPR119 Agonist C26 1353004-92-8 GPR119 agonist C26 shows potent GPR119 agonistic activity (EC50 = 42 nM, Emax = 117%) with improved liver microsome clearance than other GPR119 agonists in the series, and exerted 33% reduction in blood glucose AUC at a dose of 10 mg/kg in an oral glucose tolerance test in C57BL/6 N mice.
CSN22413 GLPG0974 1391076-61-1 GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.
CSN20362 G-1 881639-98-1 G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a Ki value of 11 nM.
CSN23532 AF64394 1637300-25-4 F64394 is an inverse agonist of GPR3 with pIC50 of 7.3.
CSN18981 Etrasimod 1206123-37-6 Etrasimod is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
CSN22390 E6130 1427058-33-0 E6130 is an orally available and highly selective CX3CR1 modulator, that may be effective for treatment of inflammatory bowel disease.
CSN22386 Dihydromunduletone 674786-20-0 Dihydromunduletone is a selective adhesion G protein–coupled receptor antagonist (aGPR) with an IC50 of ~21 μM.
CSN20481 DC260126 346692-04-4 DC260126 is antagoniat of free fatty acid receptor 1 (FFA1/GPR40) and inhibits FFA-induced the increase of intracellular Ca2+ level.
CSN20443 CYM-5541 945128-26-7 CYM-5541 is an allosteric agonist of S1P3 with EC50 of 72 nM - 132 nM.
CSN20173 Cp-154526 157286-86-7 CP-154526 is a selective, non-peptide CRF1 receptor antagonist (Ki values are 2.7 and > 10000 nM for CRF1 and CRF2 receptors respectively). CP-154526 blocks CRF-induced adenylate cyclase activation (Ki = 3.7 nM) and attenuates activation of the HPA axis by CRF.
CSN20174 CP-154526 Hydrochloride 257639-98-8 CP-154526 HCl is a selective, non-peptide CRF1 receptor antagonist (Ki values are 2.7 and > 10000 nM for CRF1 and CRF2 receptors respectively). CP-154526 HCl blocks CRF-induced adenylate cyclase activation (Ki = 3.7 nM) and attenuates activation of the HPA axis by CRF.
CSN18454 CID 16020046 834903-43-4 CID-16020046 is a selective GPR55 (LPI receptor) antagonist with IC50 of 0.15 μM.
CSN23236 CID 1375606 313493-80-0 CID 1375606 is an agonist of GPR27 (SREB1) that induces coupling of the receptor to β-arrestin 2.
CSN22239 BMS-819881 1197420-05-5 BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM. BMS-819881 also is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
CSN20202 BAR502 1612191-86-2 BAR502 is an agonist of FXR and GPBAR1 that promotes browning of white adipose tissue and reverses liver fibrosis and steatosis.
CSN20201 BAR501 1632118-69-4 BAR501 is an agonist of GPBAR1 with EC50 of 1 μM. It can effectively reduce hepatic perfusion pressure.
CSN22688 AS2034178 1030846-42-4 AS 2034178 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist.
CSN23765 AS1269574 330981-72-1 AS 1269574 is a GPR119 receptor agonist with EC50 of 2.5 μM in HEK293 cells expressing human GPR119.
CSN18543 APD597 897732-93-3 APD597 is an agonist of GPR119 with EC50 of 46 nM and is used for the treatment of type 2 diabetes.
CSN18497 AMG 837 sodium salt 865231-45-4 AMG-837 sodium is a potent GPR40 agonist (EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.
CSN22680 AMG 837 hemicalcium 1291087-14-3 AMG 837 Hemicalcium Salt is a potent free fatty acid receptor 1 (FFA1/GPR40) partial agonist with EC50 of 13.5, 22.6 and 31.7 nM at human, mouse and rat receptors, respectively.
CSN22540 AM-6226 1142222-28-3 AM-6226 is a potent and orally bioavailable GPR40 full agonist that displays efficacy in nonhuman primates. AM-6226 is the first molecule to display significant glucose lowering in cynomolgus monkeys providing additional evidence that GPR40 full agonists afford access to a powerful mechanism for maintaining glycemic control.
CSN22344 AM-1638 1142214-62-7 AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
CSN22678 AM-4668 1011531-27-3 AM 4668 is a potent FFA1 (GPR40) agonist with EC50 of 3.6 nM.
CSN21176 ALB-127158(a) 1173154-32-9 ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist.
CSN22671 AH-7614 6326-06-3 AH 7614 is a selective free fatty acid receptor 4 (FFA4/GPR120) antagonist with pIC50 of 7.1 for human FFA4.
CSN23486 3,5-Dihydroxybenzoic acid 99-10-5 3, 5-dihydroxybenzoic acid is a metabolite of alkylresinols with a certain activation effect on HCA1. It can be used as intermediates in organic synthesis.
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