Fasitibant free base

Modify Date: 2024-04-08 16:56:41

Fasitibant free base Structure
Fasitibant free base structure
Common Name Fasitibant free base
CAS Number 869939-83-3 Molecular Weight 764.78
Density N/A Boiling Point N/A
Molecular Formula C36H49Cl2N6O6S+ Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Fasitibant free base


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].

 Names

Name Fasitibant free base

 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
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
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