|(R)-2-((R)-3-(苯并[d][1,3]dioxol-5-基)-3-(6-甲氧基萘-2-磺胺基)丙酰胺基)-3-(4-(((2R,6S)-2,6-二甲基哌啶-1-基)甲基)苯基)-N-异丙基-N-甲基丙酰胺盐酸盐|CsnPharm

CAS No.: 464930-42-5

SSR240612 Catalog No. CSN21187

SSR240612 is a potent and selective non-peptide bradykinin B1 receptor antagonist with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.

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靶点选择性

生物活性

实验方案

技术信息

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]
动物研究
剂量
Mice: 1 mg/kg^[3] (i.p.), 5 mg/kg^[4] (i.p.); 10 mg/kg^[4] (p.o.) Rat: 0.3 mg/kg - 30 mg/kg^[5] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Mice: 1 mg/kg^[3] (i.p.), 5 mg/kg^[4] (i.p.); 10 mg/kg^[4] (p.o.) Rat: 0.3 mg/kg - 30 mg/kg^[5] (p.o.)
给药途径	i.p., p.o.

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2604 mL
- 6.3019 mL
- 12.6038 mL
- 5 mM
- 0.2521 mL
- 1.2604 mL
- 2.5208 mL
- 10 mM
- 0.1260 mL
- 0.6302 mL
- 1.2604 mL

技术信息

CAS号

464930-42-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C42H53ClN4O7S

运输

蓝冰

分子量

793.41

别名

溶解度

DMSO	205.0 mg/mL (258.4 mM)
Water	260.0 mg/mL (327.7 mM)

动物实验配方

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