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首页-小分子抑制剂&激动剂-GPCR-Bradykinin Receptor-SSR240612
SSR240612

Chemical Structure : SSR240612

CAS No.: 464930-42-5

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SSR240612 (SSR-240612)

货号: PC-25718Not For Human Use, Lab Use Only.

SSR240612 is a potent, selective, non-peptide antagonist of bradykinin (BK) B(1) receptor, inhibits binding of [(3)H]Lys(0)-des-Arg(9)-BK to B(1) receptor in human fibroblast MRC5 and to recombinant human B(1) receptor expressed in human embryonic kidney cells with Ki of 0.48 and 0.73 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SSR240612 is a potent, selective, non-peptide antagonist of bradykinin (BK) B(1) receptor, inhibits binding of [(3)H]Lys(0)-des-Arg(9)-BK to B(1) receptor in human fibroblast MRC5 and to recombinant human B(1) receptor expressed in human embryonic kidney cells with Ki of 0.48 and 0.73 nM, respectively.
SSR240612 has 500- to 1000-fold selectivity over B(2) receptors.
SR240612 inhibits Lys(0)-desAr(9)-BK (10 nM)-induced inositol monophosphate formation in human fibroblast MRC5 with IC50 of 1.9 nM.
SSR240612 antagonizes des-Arg(9)-BK-induced contractions of isolated rabbit aorta and mesenteric plexus of rat ileum with a pA(2) of 8.9 and 9.4, respectively.
SSR240612 inhibits des-Arg(9)-BK-induced paw edema in mice (3 and 10 mg/kg p.o. and 0.3 and 1 mg/kg i.p.).
SSR240612 reduces capsaicin-induced ear edema in mice (0.3, 3 and 30 mg/kg p.o.) and tissue destruction and neutrophil accumulation in the rat intestine following splanchnic artery occlusion/reperfusion (0.3 mg/kg i.v.).
SSR240612 inhibits thermal hyperalgesia induced by UV irradiation (1 and 3 mg/kg p.o.) and the late phase of nociceptive response to formalin in rats (10 and 30 mg/kg p.o.).
SSR240612 (20 and 30 mg/kg p.o.) prevents neuropathic thermal pain induced by sciatic nerve constriction in the rat.

物理化学性质&存储条件

分子量 793.42
分子式 C42H53ClN4O7S
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

(R)-2-((R)-3-(Benzo[d][1,3]dioxol-5-yl)-3-(6-methoxynaphthalene-2-sulfonamido)propanamido)-3-(4-(((2R,6S)-2,6-dimethylpiperidin-1-yl)methyl)phenyl)-N-isopropyl-N-methylpropanamide hydrochloride

参考文献

1. Dias JP, et al. Br J Pharmacol. 2007 Sep;152(2):280-7.

2. Gougat J, et al. J Pharmacol Exp Ther. 2004 May;309(2):661-9.

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