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hGPR91 antagonist 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
hGPR91 antagonist 1图片
CAS NO:1314796-00-3
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品名称
(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
产品介绍
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