HGPR91 antagonist 1 是小分子hGPR91选择性拮抗剂(IC50:7 μM)。
产品描述
hGPR91 antagonist 1 is a potent and selective hGPR91 antagonist (IC50: 7 μM).
体内活性
GPR91, a 7TM G-Protein-Coupled Receptor, has been recently deorphanized with succinic acid as its endogenous ligand.?Current literature indicates that GPR91 plays role in various pathophysiology including renal hypertension, autoimmune disease and retinal angiogenesis.?Starting from a small molecule high-throughput screening hit 1 (hGPR91 IC(50): 0.8 μM)-originally synthesized in Merck for Bradykinin B(1) Receptor (BK(1)R) program, systematic structure-activity relationship study led us to discover potent and selective hGPR91 antagonists e.g. 2c, 4c, and 5 g (IC(50): 7-35 nM;?>1000 fold selective against hGPR99, a closest related GPCR;?>100 fold selective in Drug Matrix screening).?Led to identification of two structurally distinct and orally bio-available lead compounds: 5g (%F: 26) and 7e (IC(50): 180 nM;?>100 fold selective against hGPR99;?%F: 87).
Cas No.
1314796-00-3
分子式
C31H23F4N3O
分子量
529.53
别名
(S)-2-(4-(1,8-萘啶-2-基)苯基)-N-(1-(4'-氟-3'-(三氟甲基)-[1,1'-联苯]-4-基)乙基)乙酰胺
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years