Dapivirine-d11(Synonyms: TMC120-d11; R147681-d11)

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Dapivirine-d11 (Synonyms: TMC120-d11; R147681-d11)

Dapivirine-d11 (TMC120-d11) 是 Dapivirine 的氘代物。Dapivirine (TMC120) 是二芳基嘧啶 (DAPY) 的原型，是具有口服活性的非核苷类逆转录酶抑制剂 (NRTI)。Dapivirine (TMC120) 可直接与 HIV 的逆转录酶结合。Dapivirine (TMC120)调节自噬并诱导 Akt、Bad 和 SAPK/JNK 的激活。

Dapivirine-d11(Synonyms: TMC120-d11; R147681-d11)

Dapivirine-d11 Chemical Structure

CAS No. : 1329613-10-6

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生物活性

Dapivirine-d11 (TMC120-d11) is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].

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

340.47

Formula

C20H8D11N5
CAS 号

1329613-10-6
中文名称

达匹维林 d11
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]. Weiwen Liu, et al. Antitumor Activity and Mechanism of a Reverse Transcriptase Inhibitor, Dapivirine, in Glioblastoma. J Cancer. 2018 Jan 1;9(1):117-128.

    [3]. Bríd Devlin, et al. Development of dapivirine vaginal ring for HIV prevention. Antiviral Res. 2013 Dec;100 Suppl:S3-8.

    [4]. Yven Van Herrewege, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9.

    [5]. Michael E Halwes, et al. Pharmacokinetic modeling of a gel-delivered dapivirine microbicide in humans. Eur J Pharm Sci. 2016 Oct 10;93:410-8.

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