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编 号:F364191
分子式:C17H18N4O2
分子量:310.35
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC50=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains.

体内研究:
Lersivirine (oral gavage; 0, 150, 350, and 500 mg/kg; once daily; gestation days 6 to 17, followed by cesarean section on gestation day 18. ) allows induction of hepatic metabolizing enzymes at the first 2 days at 250 mg/kg, after which the dose is increased to 500 mg/kg/day in Mated Crl:CD1(ICR) mice. Lersivirine leads to skeletal variations which related to delayed development and decreased fetal ossifications.

体外研究:
Lersivirine demonstrates excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes.
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