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Fasitibant chloride hydrochloride

CAS No. : 869880-33-1

MCE 站：Fasitibant chloride hydrochloride

产品活性：Fasitibant chloride hydrochloride (MEN16132) 是一种强效、选择性、高亲和力、长效的非肽性缓激肽 B₂ 受体 (BK₂receptor) 拮抗剂。Fasitibant 具有促炎作用，可用于骨关节炎和类风湿关节炎的研究等。

研究领域：GPCR/G Protein

作用靶点：Bradykinin Receptor

In Vitro: Fasitibant exhibits high affinity for the BK binding site, pK_i values 8.9 in intact cells and 10.17-K_i 0.067 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, pIC₅₀ 8.1 and 8.4, respectively).
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.
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.

In Vivo: Fasitibant chloride hydrochloride (injection into the knee joint?;100 ?g 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.

相关产品：Bradykinin  |  Icatibant  |  [Des-Arg9]-Bradykinin acetate  |  ELN-441958  |  Lys-[Des-Arg9]Bradykinin TFA  |  Bradykinin (2-9)  |  Bradykinin (1-5)  |  Bradykinin (1-6)  |  Retrobradykinin  |  [Hyp3]-Bradykinin  |  Bradykinin (1-3)  |  Bradykinin (1-7)  |  FR167344 free base

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