货号:A306689
同义名:
UK-453061;UK-453,061
Lersivirine是一种下一代非核苷类逆转录酶抑制剂(NNRTI,IC50 = 119 nM),具有独特的耐药特征,对野生型人类免疫缺陷病毒(HIV)和临床相关的 NNRTI 抵抗株表现出强效的抗逆转录病毒活性。
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描述 | Lersivirine (UK-453061) is a potent and selective non-nucleoside reverse transcription inhibitor (NNRTI) with an IC50 of 119 nM, showing high efficacy against NNRTI-resistant viruses. It demonstrates strong antiretroviral effects against both wild-type HIV and clinically relevant NNRTI-resistant strains[1]. |
体内研究 | Lersivirine, administered via oral gavage at doses of 0, 150, 350, and 500 mg/kg daily from gestation days 6 to 17, followed by cesarean section on day 18, induces hepatic metabolizing enzymes initially at 250 mg/kg, later increased to 500 mg/kg/day in mated Crl:CD1(ICR) mice. This treatment is associated with skeletal variations indicative of delayed development and reduced fetal ossifications[1]. |
体外研究 | Lersivirine shows remarkable efficacy against extensive panels of both wild type and drug-resistant HIV, aligning with its positive results against isolated RT enzymes[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.22mL 0.64mL 0.32mL |
16.11mL 3.22mL 1.61mL |
32.22mL 6.44mL 3.22mL |
CAS号 | 473921-12-9 |
分子式 | C17H18N4O2 |
分子量 | 310.35 |
别名 | UK-453061;UK-453,061 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Room Temperature |
溶解方案 |
DMSO: 50 mg/mL(161.11 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |