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编 号：F489030
分子式：C36H50Cl4N6O6S
分子量：836.7
分子式：C36H50Cl4N6O6S
分子量：836.7
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CAS No: 869880-33-1
产品详情
生物活性：
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2)?receptor antagonist. Fasitibant chloride hydrochloride has?proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.
体内研究：
Fasitibant chloride hydrochloride (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。Animal Model:Male wistar rats?with inflammatory arthritis
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
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.
体外研究：
Fasitibant chloride hydrochloride (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。
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2)?receptor antagonist. Fasitibant chloride hydrochloride has?proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.
体内研究：
Fasitibant chloride hydrochloride (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。Animal Model:Male wistar rats?with inflammatory arthritis
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
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.
体外研究：
Fasitibant chloride hydrochloride (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。
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