产品
编 号:F762808
分子式:C14H13FN4O
分子量:272.28
产品类型
结构图
CAS No: 3032452-65-3
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产品详情
生物活性:
NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively.
体内研究:
NPD-2975 (25 mg/kg,每日2次,连用5天;灌胃) 提高了 HAT 感染小鼠模型中 i 期的存活率。NPD-2975 在小鼠中的药代动力学分析RouteDose (mg/kg)Tmax (h)Cmax (μM)T1/2 (h)AUC0-6 h (ng·h/mL)Cl (mL/min)
PO5015.253.466064.7558.5
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