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  • Doravirine
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Doravirine

A non-nucleoside reverse transcriptase inhibitor

原价
¥762-9712
价格
610-7770
Doravirine的二维码

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  • 货号: ajci22494
  • CAS: 1338225-97-0
  • 别名: 多拉维林; MK-1439
  • 分子式: C17H11ClF3N5O3
  • 分子量: 425.75
  • 纯度: >98%
  • 溶解度: DMSO : ≥ 30 mg/mL (70.46 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

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]

参考文献:
[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.

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