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• 產(chǎn)品描述： Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively

• 靶點： IC50: 4.5 nM (wild type reverse transcriptase); 5.5 nM ( K103N reverse transcriptase); 6.1 nM (Y181C reverse transcriptase);HIVProtease;?ReverseTranscriptase

• 體外研究：
  Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitors with minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses)

• 體內(nèi)研究：
  Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax

• 參考文獻(xiàn)：
  1. Lai MT et al. In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2014;58(3):1652-63. 2. Anderson MS et al. Safety, tolerability and pharmacokinetics of doravirine, a novel HIV non-nucleoside reverse transcriptase inhibitor, after single and multiple doses in healthy subjects. Antivir Ther. 2015;20(4):397-405.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.349 ml	11.744 ml	23.488 ml
  5 mM	0.47 ml	2.349 ml	4.698 ml
  10 mM	0.235 ml	1.174 ml	2.349 ml
  50 mM	0.047 ml	0.235 ml	0.47 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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