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• 产品描述： DPC-681 is a potent and selective HIV protease inhibitor (IC90s: 4 to 40 nM for wild-type HIV-1).

• 体外研究：
  DPC 681 displays no loss in potency toward recombinant mutant HIVs with the D30N mutation and a fivefold or smaller loss in potency toward mutant variants with three to five amino acid substitutions. When all of the HIV-1 strains tested are considered, the average concentrations required for 90% inhibition of replication were 7.3 ± 3.4 for DPC 681.

• 体内研究：
  The total body clearance (CL) of DPC 681 in dogs was high (1.8 liters/h/kg) equaling hepatic blood flow for this species (1.8 liters/h/kg). The Cmax increased ninefold between the 10- and 30-mg/kg DPC 681 dose groups. Bioavailability also increased between the 10- and 30-mg/kg dose groups (18.3 and 78.1%, respectively), after oral dosing. These data show that hepatic extraction (first-pass effect) can be saturated in the dog

• 参考文献：
  1. Kaltenbach RF 3rd, et al. DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. Antimicrob Agents Chemother. 2001 Nov;45(11):3021-8.

• 溶解性： 10  mM  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.493 ml	7.464 ml	14.929 ml
  5 mM	0.299 ml	1.493 ml	2.986 ml
  10 mM	0.149 ml	0.746 ml	1.493 ml
  50 mM	0.03 ml	0.149 ml	0.299 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 *