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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. |