1157852-02-2
Chemical Structure
Fasitibant chloride
Synonym(s): MEN16132 free base
- CAS No.: 1157852-02-2
- Formula:C36H49Cl3N6O6S
- Molecular Weight:800.23
IUPAC Name: (S)-4-amino-5-(4-(4-((2,4-dichloro-3-(((2,4-dimethylquinolin-8-yl)oxy)methyl)phenyl)sulfonamido)tetrahydro-2H-pyran-4-carbonyl)piperazin-1-yl)-N,N,N-trimethyl-5-oxopentan-1-aminium chloride
InChIKey: ZNHJDJYKDVGQSH-JMAPEOGHSA-M
SMILES: O=C(N(CC1)CCN1C([C@@H](N)CCC[N+](C)(C)C)=O)C2(CCOCC2)N[S](=O)(C(C=CC(Cl)=C3COC4=CC=CC(C(C)=C5)=C4N=C5C)=C3Cl)=O.[Cl-]
Biological Activity: 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].
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Fasitibant chloride | 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. | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
