CAS NO: | 869880-33-1 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
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].
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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. |