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编 号:F755944
分子式:C19H18N3O2PS
分子量:383.4
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis.

体内研究:
Zharp2-1(15 mg/kg;灌胃;每天一次,持续 6 天)可保护大鼠免受 DNBS 诱导的结肠缩短和结肠重量增加,保护大鼠免受 DNBS 诱导的腹泻。Zharp2-1 显著改善结肠粘膜结构破坏、肌肉增厚和炎症浸润。药代动力学分析RouteDose (mg/kg)T1/2 (h)Tmax (h)Cmax (ng·h/mL)AUC (ng·h/mL)Vd (L/kg)Cl (mL/kg/min)F (%)
Mouseiv21.229891.111.1
po100.5961019,236129
Rativ21.778890.64.2
po103.3332318,80348
Dogiv12.116451.79.5
po50.7219210,800131

体外研究:
Zharp2-1 (IC50=6.4-17.4 nM; 2 h) 预处理 THP-1 和 iBMDM 细胞,并抑制 10 μg/mL MDP 或 1 μg/mL L18-MDP 诱导 12 小时后引起的 IL-6 和 TNF-α 释放。
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