Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and longlasting nonpeptidebradykinin B₂(BK₂) receptorantagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis, et al^[1].

IC50: Bradykinin B2 Receptor^[1]

Fasitibant exhibits high affinity for the BK binding site, pK_ivalues 8.9 in intact cells and 10.17-K_i0.067 nM in cell membrane in synovial cells.Fasitibant also echibits high antagonist potency in blocking the effects produced by BK in these cells both after 1 h-(phospholipase C activation, pK_B=9.9) and 24 h-incubation (release of IL-6 and IL-8, pIC₅₀8.1 and 8.4, respectively)^[1].
Fasitibant chloride hydrochloride (1 μM; 30 min preincubation before BK) prevents BK-induced sustained production of PGE2 and transient COX-2 gene expression in synovial fibroblasts^[1].
Fasitibant chloride hydrochloride completely prevents the potentiating effect of BK on IL-1β, both in terms of PGE2 production and COX-2 gene expression in synovial fibroblasts^[1].

Fasitibant chloride hydrochloride (injection into the knee joint ;100 μg per knee; combines with dexamethasone) is more effective than each agent administered alone in inhibiting knee joint inflammation and release of inflammatory mediators. Fasitibant chloride alone reaches a comparable maximal inhibitory effect of about 40–45% on the carrageenan-induced joint pain, however, Combination administration achieves full inhibition in male Wistar rats with inflammatory arthritis^[2].

836.70

C₃₆H₅₀Cl₄N₆O₆S

869880-33-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.