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首页-小分子抑制剂&激动剂-GPCR-Bradykinin Receptor-FR173657
FR173657

Chemical Structure : FR173657

CAS No.: 167838-64-4

FR173657 (FK-3657)

货号: PC-26638Not For Human Use, Lab Use Only.

FR173657 (FK-3657) is a potent, selective, orally active bradykinin B2 receptor (B2R) antagonist with IC50 of 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

FR173657 (FK-3657) is a potent, selective, orally active bradykinin B2 receptor (B2R) antagonist with IC50 of 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively.
FR173657 displaces[3H]-BK binding to B2 receptors with an IC50 of 2.9 nM and a Ki of 0.36 nM in human lung fibroblast IMR-90 cells.
FR173657 doess not reduce [3H]-des]Arg10-kallidin binding to B1 receptors.
FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg).
FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg).

物理化学性质&存储条件

分子量 592.48
分子式 C30H27Cl2N5O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-3-(6-Acetamidopyridin-3-yl)-N-(2-((2,4-dichloro-3-(((2-methylquinolin-8-yl)oxy)methyl)phenyl)(methyl)amino)-2-oxoethyl)acrylamide

参考文献

1. Asano M, et al. Br J Pharmacol. 1997 Feb;120(4):617-24.

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