1157852-02-2

1157852-02-2 structure

Name: Fasitibant chloride
Chemical Name: [(4S)-4-amino-5-[4-[4-[[2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]phenyl]sulfonylamino]oxane-4-carbonyl]piperazin-1-yl]-5-oxopentyl]-trimethylazanium
CAS Number: 1157852-02-2
Molecular Formula: C₃₆H₄₉Cl₃N₆O₆S
Molecular Weight: 764.78200
Catalog: Signaling Pathways GPCR/G Protein Bradykinin Receptor
Create Date: 2017-11-06 15:25:28
Modify Date: 2024-01-07 16:34:45
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].

Name	[(4S)-4-amino-5-[4-[4-[[2,4-dichloro-3-[(2,4-dimethylquinolin-8-yl)oxymethyl]phenyl]sulfonylamino]oxane-4-carbonyl]piperazin-1-yl]-5-oxopentyl]-trimethylazanium
Synonyms	Fasitibant chloride UNII-0WL827Z7AE Fasitibant UNII-7J764K70IG

Description	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].
Related Catalog	Research Areas >> Cardiovascular Disease Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Bradykinin Receptor
Target	B2R[1][2]
In Vitro	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).
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: 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%.
References	[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.

Molecular Formula	C₃₆H₄₉Cl₃N₆O₆S
Molecular Weight	764.78200
Exact Mass	763.28100
PSA	152.54000
LogP	6.09720

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