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Product 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].
Web ID
– HY-14886
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C36H49Cl3N6O6S
References
– [1]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.|[2]Claudio Valenti, et al. Fasitibant Chloride, a Kinin Bâ‚‚ Receptor Antagonist, and Dexamethasone Interact to Inhibit Carrageenan-Induced Inflammatory Arthritis in Rats. Br J Pharmacol. 2012 Jun;166(4):1403-10.|[3]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.
CAS Number
– 1157852-02-2
Molecular Weight
– 800.23
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-]
Clinical Information
– Phase 2
Research Area
– Neurological Disease; Cardiovascular Disease
Solubility
– 10 mM in DMSO
Target
– Bradykinin Receptor
Isoform
– Bradykinin B2 Receptor (B2R)
Pathway
– GPCR/G Protein
Product type
– Reference compound
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