Fasitibant free base

Names

[ CAS No. ]:
869939-83-3

[ Name ]:
Fasitibant free base

Biological Activity

[Description]:

Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis[1].

[Related Catalog]:

Research Areas >> Metabolic Disease
Signaling Pathways >> GPCR/G Protein >> Bradykinin Receptor

[Target]

Bradykinin B2 Receptor (B2R)


[In Vitro]

Fasitibant (free base) (1 µM；30 min) 减少了滑膜细胞中 BK 诱导的 PGE2 形成和 COX-2 基因表达[1]。

[In Vivo]

Fasitibant (free base) (100 µg；膝盖注射；单剂量) 显著降低了大鼠中卡拉胶 (Carrageenan，HY-125474) 诱导的 IL-1b、IL-6、GRO/CINC-1 滑膜细胞因子的释放，PGE 代谢产物的形成，髓过氧化物酶 (MPO) 的活性，当与地塞米松 (Dexamethasone，HY-14648) 联用时效果更显著[2]。

[References]

[1]. S Meini, et al. Fasitibant prevents the bradykinin and interleukin 1β synergism on prostaglandin E₂ release and cyclooxygenase 2 expression in human fibroblast-like synoviocytes. Naunyn Schmiedebergs Arch Pharmacol. 2012 Aug;385(8):777-86.  

[2]. 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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C36H49Cl2N6O6S+

[ Molecular Weight ]:
764.78

Related Compounds