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Doravirine

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Chemical Structure| 1338225-97-0 同义名 : 多拉维林（MK-1439） ;MK-1439
CAS号 : 1338225-97-0
货号 : A367825
分子式 : C17H11ClF3N5O3
纯度 : 99%+
分子量 : 425.749
MDL号 : MFCD22417167
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(246.62 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：
生物活性
描述 Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 12, 9.7 and 9.7nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively. Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitor 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[3]. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses). 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[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.23mL

11.74mL

2.35mL

1.17mL

23.49mL

4.70mL

2.35mL
参考文献

[1]Feng M, Sachs NA, et al. Doravirine Suppresses Common Nonnucleoside Reverse Transcriptase Inhibitor-Associated Mutants at Clinically Relevant Concentrations. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2241-7.

[2]Lai MT, Feng M, et al. In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2014;58(3):1652-63.

[3]Lai MT, Feng M, Falgueyret JP, et al. In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2014;58(3):1652-1663.

[4]Anderson MS, Gilmartin J, Cilissen C, 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.