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Fasitibant chloride

产品编号 T38544 CAS 1157852-02-2

别名: MEN16132 free base, Fasitibant chloride

Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis.

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Fasitibant chloride, CAS 1157852-02-2

规格	价格/CNY		货期	数量
25 mg	￥ 10,600		待询

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其他形式的 Fasitibant chloride:

Fasitibant chloride hydrochloride
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Fasitibant
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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Fasitibant chloride (MEN16132 free base) is a powerful and specific nonpeptide antagonist of the bradykinin B2 receptor (B2R). This compound effectively reduces joint pain and mitigates joint edema in a rat model of Carrageenan-induced arthritis.
体外活性	Fasitibant chloride (MEN16132 free base; 1 μM; pre-treatment 30 min before BK) produces a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation[2]. Fasitibant chloride inhibits the phosphorylation of FRSα, ERK1/2, STAT3 (BK induced; 1 μM; for 15 min), except AKT in HUVEC[2]. Cell Viability Assay[2]Cell Line: human umbilical vein endothelial cells (HUVEC) Concentration: 1 μM Incubation Time: Pre-treatment 30 min before Bradykinin (BK; 1 μM; for 24 h) Result: Produced a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation (without affecting FGFR-2 activity).
体内活性	Fasitibant chloride (MEN16132 free base; 100 μg per knee; injection into the knee; 30 min before λ-carrageenan) inhibits about 40-45% on the carrageenan-induced joint pain and knee joint oedema[1]. Animal Model: Male Wistar rats weighing 250-300 g[1]Dosage: 100 μg per knee Administration: Injection into the knee; 30 min before λ-carrageenan Result: Inhibited about 40-45% on the carrageenan-induced joint pain and knee joint oedema. Reduced the neutrophil infiltration in the synovium by about 60% and the release of prostaglandins by about 30%.

别名	MEN16132 free base, Fasitibant chloride
分子量	800.23
分子式	C36H49Cl3N6O6S
CAS No.	1157852-02-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Claudio Valenti, et al. Fasitibant Chloride, a Kinin B₂ Receptor Antagonist, and Dexamethasone Interact to Inhibit Carrageenan-Induced Inflammatory Arthritis in Rats. Br J Pharmacol. 2012 Jun;166(4):1403-10. 2. Erika Terzuoli, et al. Bradykinin B2 Receptor Contributes to Inflammatory Responses in Human Endothelial Cells by the Transactivation of the Fibroblast Growth Factor Receptor FGFR-1. Int J Mol Sci. 2018 Sep 6;19(9):2638. 3. Paola Cucchi, et al. MEN16132, a Novel Potent and Selective Nonpeptide Antagonist for the Human Bradykinin B2 Receptor. In Vitro Pharmacology and Molecular Characterization. Eur J Pharmacol. 2005 Dec 28;528(1-3):7-16.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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