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Doravirine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Doravirine图片
CAS NO:1338225-97-0
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Doravirine (MK-1439) 是一种高度特异性的 HIV-1 非核苷类逆转录酶抑制剂,对野生型和 K103N 和 Y181C 逆转录酶突变体的 IC50 分别为 4.5 nM、5.5 nM 和 6.1 nM 。
Cas No.1338225-97-0
别名多拉维林; MK-1439
Canonical SMILESN#CC1=CC(OC2=C(C(F)(F)F)C=CN(CC(N3C)=NNC3=O)C2=O)=CC(Cl)=C1
分子式C17H11ClF3N5O3
分子量425.75
溶解度DMSO : ≥ 30 mg/mL (70.46 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Doravirine is a novel non-nucleoside inhibitor of HIV-1 reverse transcriptase with potent activity against wild-type virus (95% inhibitory concentration 19 nM, 50% human serum). target:HIV [1]In vitro: Doravirine exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with IC50 value of 12, 21, 31, and 33 nM, respectively. [1] MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).[2]In vivo: Administration of 50 mg doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity (AUC0-∞) and C24 h with no change in Cmax. Midazolam AUC0-∞ is slightly reduced by coadministration of doravirine (geometric mean ratio 0.82, 90% CI 0.70, 0.97). [3]

References:
[1]. Feng M 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 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]. 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.