PNU-103017
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| 包装规格: | 100mg in glass bottle |
| 产品描述: | 基本信息 产品编号:P11348 产品名称:PNU-103017 CAS: 166335-18-8 储存条件 粉末 -20℃ 四年 分子式: C28H28N2O5S 分子量 504.60 化学名: 4-Cyano-N-(3-(cyclopropyl(5,6,7,8,9,10-hexahydro-4-hydroxy-2-oxo-2H-cycloocta(b)pyran-3-yl)methyl )phenyl)benzenesulfonamide Solubility (25°C) 体外 DMSO Ethanol Water 体内 现配现用 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 生物活性 产品描述 一种 HIV 蛋白酶抑制剂。 靶点/IC50 HIV protease 体内研究 PNU-103017 is a selective HIV aspartyl protease inhibitor under evaluation as a potential oral treatment of Acquired Immunodeficiency Diseases. PNU-103017 is a racemic mixture of two enantiomers, designated PNU-103264 (R-) and PNU103265 (S-). The Cmax (P≤0.0349), Cmin (P≤0.0168), and Cav (P≤0.0118) are significantly higher for the (R)- than the (S)-enantiomer, showing enantioselective pharmacokinetics of PNU-103017 in the dog. 推荐实验方法(仅供参考) 动物实验: Animal Administration Rats and dogs are used in this study. In preclinical toxicology studies, dogs (three per gender per dose) receive 50, 100, 200,or 250 mg/kg/day, and rats (three per gender per dose) receive 80, 240, or 720 mg/kg/day PNU-103017 in a 0.5 N sodium hydroxide aqueous solution orally, twice daily, 8 and 16 h apart, respectively, for 14 days. Sequential blood specimens are collected at 0 (prior to the first daily dosing), 1, 2, 4, 8 (prior to the second daily dosing), 9, 10, 12, 16 (for dog only), and 24 h after the first daily dosing on treatment days 1, 8, and 14 for the dog and rat studies. The samples are placed into heparinized tubes, and the plasma is separated by centrifugation and stored at or below -10°C until analysis. |
| 保存条件: | -20℃ |
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