Doravirine (MK-1439) 是一种高度特异性的 HIV-1 非核苷逆转录酶抑制剂，对野生型以及 K103N 和 Y181C 逆转录酶突变体的 IC₅₀ 值分别为 4.5 nM，5.5 nM 和 6.1 nM。

Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC 50 s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively.

Solid

IC50: 4.5 nM (wild type reverse transcriptase); 5.5 nM ( K103N reverse transcriptase); 6.1 nM (Y181C reverse transcriptase)

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). has not independently confirmed the accuracy of these methods. They are for reference only.

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 C max . has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (234.88 mM; Need ultrasonic)配制储备液