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• 产品描述： 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

• 靶点： IC50: 119 nM (NNRT);HIVProtease;ReverseTranscriptase

• 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

• 参考文献：
  1. Mowbray CE, et al. Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5857-60. 2. Gregg D Cappon, et al. Developmental toxicity study of lersivirine in mice. Birth Defects Res B Dev Reprod Toxicol. 2012 Jun;95(3):225-30.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.222 ml	16.111 ml	32.222 ml
  5 mM	0.644 ml	3.222 ml	6.444 ml
  10 mM	0.322 ml	1.611 ml	3.222 ml
  50 mM	0.064 ml	0.322 ml	0.644 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *