Fasitibant (chloride)
CAS No. : 1157852-02-2
(Synonyms: MEN16132 (free base))
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| Cat. No. : | HY-14886 |
| M.Wt: | 800.23 |
| Formula: | C36H49Cl3N6O6S |
| Purity: | >98 % |
| Solubility: | 10 mM in DMSO |
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].
IC50 & 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].
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].
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