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编 号：F540643
分子式：C16H16N2
分子量：236.31
分子式：C16H16N2
分子量：236.31
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CAS No: 960119-75-9
产品详情
生物活性：
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium?(DSS; HY-116282C)-induced murine experimental colitis.
体内研究：
Fc 11a-2 (3-30 mg/kg; 口服; 从第 1 天到第 10 天) 剂量依赖性地减轻由 DSS 诱导的体重减轻和结肠长度缩短。Animal Model:C57BL/6 mice induced Colitis with 2.5% DSS
Dosage:3, 10, 30 mg/kg
Administration:Orally; from day 1 to day 10
Result:Significantly attenuated the loss of body weight during the disease progression at 10 and 30 mg/kg. The myeloperoxidase (MPO) activity in colons at 10 and 30 mg/kg was lower than that of the vehicle-treated group. Significantly reduced the disease activity index, histopathologic scores and myeloperoxidase activity.
体外研究：
Fc 11a-2 (10 μM) 抑制用 ATP 激活的 LPS?(HY-D1056) 引发的 THP-1 细胞中释放 IL-1β 和 IL-18，IC50 约 10 μM。
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium?(DSS; HY-116282C)-induced murine experimental colitis.
体内研究：
Fc 11a-2 (3-30 mg/kg; 口服; 从第 1 天到第 10 天) 剂量依赖性地减轻由 DSS 诱导的体重减轻和结肠长度缩短。Animal Model:C57BL/6 mice induced Colitis with 2.5% DSS
Dosage:3, 10, 30 mg/kg
Administration:Orally; from day 1 to day 10
Result:Significantly attenuated the loss of body weight during the disease progression at 10 and 30 mg/kg. The myeloperoxidase (MPO) activity in colons at 10 and 30 mg/kg was lower than that of the vehicle-treated group. Significantly reduced the disease activity index, histopathologic scores and myeloperoxidase activity.
体外研究：
Fc 11a-2 (10 μM) 抑制用 ATP 激活的 LPS?(HY-D1056) 引发的 THP-1 细胞中释放 IL-1β 和 IL-18，IC50 约 10 μM。
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