产品
编 号:F407794
分子式:C22H21N3O3
分子量:375.42
产品类型
结构图
CAS No: 620175-39-5
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产品详情
生物活性:
AFN-1252 is an orally active and selective inhibitor of FabI, an essential enzyme in fatty acid biosynthesis in Staphylococcus spp. AFN-1252 exhibits exquisite and highly selective activity against Staphylococcus spp. AFN-1252 exhibits typical MIC90 values of ?0.015 μg/ml against diverse clinical isolates of S. aureus. AFN-1252 is efficacious in a mouse model of septicemia providing 100% protection from an otherwise lethal peritoneal infection of S. aureus Smith.
体内研究:
AFN-1252 (0.03-3 mg/kg;口服灌胃;单剂量) 对败血症小鼠模型有效,单次口服剂量 1 mg/kg 可获得 100% 存活率。Animal Model:Female 5- to 6-week-old CD-1 mice (18 to 22 g) with S. aureus Smith bacterial inoculum
Dosage:0.03, 0.1, 0.3, 1, 3 mg/kg
Administration:Oral gavage; single dose
Result:Was efficacious in a mouse model of septicemia, with 100% survival obtained with a single oral dose of 1 mg/kg. The calculated ED50s (95% confidence limits) were 0.15 (0.11 to 0.21) mg/kg.
体外研究:
AFN-1252 对临床分离的金黄色葡萄球菌 (MIC90=0.015 μg/ml) 和凝固酶阴性葡萄球菌 (MIC90=0.12 μg/ml) 非常有效