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Fasitibant chloride hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fasitibant chloride hydrochloride图片
CAS NO:869880-33-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
MEN16132
产品介绍
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。
生物活性

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& Target

IC50: Bradykinin B2 Receptor[1]

体外研究
(In Vitro)

Fasitibant exhibits high affinity for the BK binding site, pKivalues 8.9 in intact cells and 10.17-Ki0.067 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, pKB=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].

体内研究
(In Vivo)

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].

Animal Model:Male wistar rats with inflammatory arthritis[2]
Dosage:100 μg per knee
Administration:Injection into the knee joint; 100 μg per knee; combines with dexamethasone
Result:Was more effective than each drug administered alone in inhibiting knee joint inflammation.
Reduced joint pain and diminished joint oedema.
Animal Model:Male Wistar rats with inflammatory arthritis[2]
Dosage:100 μg per knee
Administration:Injection into the knee joint; 100 μg per knee; combines with dexamethasone
Result:Was more effective than each drug administered alone in inhibiting knee joint inflammation.
Reduced joint pain and diminished joint oedema.
Clinical Trial
分子量

836.70

Formula

C36H50Cl4N6O6S

CAS 号

869880-33-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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