1、分子量373.38 溶解性(25C) DMSO 分子式C H N O SWater CAS号909859-19-4Ethanol 储存条件3年 -20C 粉末状 生物活性 SID 852843 is an inhibitor of West Nile Virus NS2B-NS3 proteinase. Flaviviruses, such as West Nile and Dengue, are a threat to humans from both public health and bioterrorism perspectives. The NS3 proteinase is ess
2、ential for flaviviral maturation. Inhibitors of NS3 are sought for treatment and prophylactic therapeutics. The NIH molecular library was screened for activity against West Nile Virus NS3, resulting in the discovery of SID 852843. This compound inhibits the NS3 proteinase of West Nile, but not of De
3、ngue type 2 virus. SID 852843 is a reversible, allosteric inhibitor of the formation of the functional conformation of the NS3 proteinase. This is the first flaviviral proteinase inhibitor with the potential to lead to a drug. Aprotinin is an efficient inhibitor of NS3, but it is not selective and h
4、as low penetration into cells, limiting its potential for therapeutic use. 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南) 小鼠大鼠兔豚鼠仓鼠狗 重量 (kg)0.020.151.80.40.0810 体表面积 (m )0.0070.0250.150.050.020.5 K 系数36128520 动物 A (mg/kg) = 动物 B (mg/kg) 动物 B的K 系数 动物 A的K 系数 例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的K 系数(3),再除以大鼠的K 系数(6), 得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。 SID 852843 目录号M8171 化学数据 171535 2 m m m mm