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SSR240612

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Chemical Structure| 464930-42-5 同义名 : -
CAS号 : 464930-42-5
货号 : A612447
分子式 : C42H53ClN4O7S
纯度 : 98%
分子量 : 793.411
MDL号 : MFCD09260115
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(63.02 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 SSR240612 is a novel non-peptide antagonist of the bradykinin B1 receptor, with 500-1,000 fold selectivity for B1 over B2. It could inhibit the binding of peptide [3H]Lys0-des-Arg9-BK to bradykinin B1 receptor with Ki values of 0.48 and 0.73 nM for human fibroblast MRC5 and human embryonic kidney cells expressing recombinant human B1 receptor, respectively. SSR240612 antagonized Lys0-desAr9-BK both in vitro and in vivo. It inhibited Lys0-desAr9-BK-induced inositol monophosphate formation in MRC5 with an IC50 of 1.9 nM. Administration of SSR240612 at dose of 3 and 10 mg/kg p.o., or 0.3 and 1 mg/kg i.p., inhibited desAr9-BK-induced paw edema in mice[1]. Oral administration of SSR240612 at dose of 10mg/kg once daily for 7 days reversed low state inflammation in adipose tissue and plasma fatty acids changes associated with insulin resistance in glucose-fed rats[2].
作用机制 SSR240612 is a competitive inhibitor of bradykinin B1 receptor.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.26mL

0.25mL

0.13mL

6.30mL

1.26mL

0.63mL

12.60mL

2.52mL

1.26mL
参考文献

[1]Gougat J, Ferrari B, et al. SSR240612 [(2R)-2-[((3R)-3-(1,3-benzodioxol-5-yl)-3-[[(6-methoxy-2-naphthyl)sulfonyl]amino]propanoyl)amino]-3-(4-[[2R,6S)-2,6-dimethylpiperidinyl]methyl]phenyl)-N-isopropyl-N-methylpropanamide hydrochloride], a new nonpeptide antagonist of the bradykinin B1 receptor: biochemical and pharmacological characterization. J Pharmacol Exp Ther. 2004 May;309(2):661-9. Epub 2004 Jan 27.

[2]Dias JP, Couture R, et al. Blockade of kinin B(1) receptor reverses plasma fatty acids composition changes and body and tissue fat gain in a rat model of insulin resistance. Diabetes Obes Metab. 2012 Mar;14(3):244-53.