Fasitibant chloride_product_DataBase

Bioactivity	Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model[1][2][3].
Target	B2R
Invitro	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:
In Vivo	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:
Name	Fasitibant chloride
CAS	1157852-02-2
Formula	C36H49Cl3N6O6S
Molar Mass	800.23
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB

Fasitibant chloride

CAS: 1157852-02-2 F: C36H49Cl3N6O6S W: 800.23