(Rac)-Efavirenz-d4

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
(Rac)-Efavirenz-d4 

(Rac)-Efavirenz-d4 ((Rac)-DMP 266-d4) 是 Efavirenz 氘代消旋体。Efavirenz (DMP 266) 是一种有效的野生型 HIV-1 RT 抑制剂，Ki 为 2.93 nM，抑制 HIV-1 复制，IC95 为 1.5 nM。

(Rac)-Efavirenz-d4

(Rac)-Efavirenz-d4 Chemical Structure

CAS No. : 1246812-58-7

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生物活性

(Rac)-Efavirenz-d4 ((Rac)-DMP 266-d4) is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

319.70

Formula

C14H5D4ClF3NO2
CAS 号

1246812-58-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Young SD, et al. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1995 Dec;39(12):2602-5.

    [3]. Held DM, et al. Differential susceptibility of HIV-1 reverse transcriptase to inhibition by RNA aptamers in enzymatic reactions monitoring specific steps during genome replication. J Biol Chem. 2006 Sep 1;281(35):25712-22.

    [4]. Grobler JA, et al. HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. J Biol Chem. 2007 Mar 16;282(11):8005-10.

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