产品
编 号：F665480
分子式：C36H49Cl3N6O6S
分子量：800.23
分子式：C36H49Cl3N6O6S
分子量：800.23
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CAS No: 1157852-02-2
产品详情
生物活性：
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.
体内研究：
Fasitibant chloride (MEN16132 free base; 100 μg per knee; injection into the knee; 30 min before λ-carrageenan) inhibits about 40-45% on the carrageenan-induced joint pain and knee joint oedema. Animal Model:Male Wistar rats weighing 250-300 g
Dosage:100 μg per knee
Administration:Injection into the knee; 30 min before λ-carrageenan
Result:Inhibited about 40-45% on the carrageenan-induced joint pain and knee joint oedema. Reduced the neutrophil infiltration in the synovium by about 60% and the release of prostaglandins by about 30%.
体外研究：
Fasitibant chloride (MEN16132 free base; 1 μM; pre-treatment 30 min before BK) produces a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation. Fasitibant chloride inhibits the phosphorylation of FRSα, ERK1/2, STAT3 (BK induced; 1 μM; for 15 min), except AKT in HUVEC.
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.
体内研究：
Fasitibant chloride (MEN16132 free base; 100 μg per knee; injection into the knee; 30 min before λ-carrageenan) inhibits about 40-45% on the carrageenan-induced joint pain and knee joint oedema. Animal Model:Male Wistar rats weighing 250-300 g
Dosage:100 μg per knee
Administration:Injection into the knee; 30 min before λ-carrageenan
Result:Inhibited about 40-45% on the carrageenan-induced joint pain and knee joint oedema. Reduced the neutrophil infiltration in the synovium by about 60% and the release of prostaglandins by about 30%.
体外研究：
Fasitibant chloride (MEN16132 free base; 1 μM; pre-treatment 30 min before BK) produces a consistent reduction of the FGF-2 expression (BK induced) and decrement of BK induced-FGFR-1 phosphorylation. Fasitibant chloride inhibits the phosphorylation of FRSα, ERK1/2, STAT3 (BK induced; 1 μM; for 15 min), except AKT in HUVEC.
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