Tipranavir-d4(Synonyms: 替拉那韦 d4)

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Tipranavir-d4 (Synonyms: 替拉那韦 d4)

Tipranavir-d4 (PNU-140690-d4) 是 Tipranavir 的氘代物。Tipranavir (PNU-140690) 有效抑制 HIV-1 蛋白酶 酶活性和二聚化，对抗多种蛋白酶抑制剂(PI)的HIV-1分离株具有有效的活性，IC50 为 66-410 nM。Tipranavir 抑制 SARS-CoV-2 3CLpro 活性。

Tipranavir-d4(Synonyms: 替拉那韦 d4)

Tipranavir-d4 Chemical Structure

CAS No. : 1217819-15-2

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生物活性

Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM[1][2]. Tipranavir inhibits SARS-CoV-2 3CLpro activity[3].

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

606.69

Formula

C31H29D4F3N2O5S
CAS 号

1217819-15-2
中文名称

替拉那韦 d4
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]. Aoki M, et al. Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1. J Virol. 2012 Dec;86(24):13384-96.

    [3]. Li F, et al. Metabolism-mediated drug interactions associated with ritonavir-boosted tipranavir in mice. Drug Metab Dispos. 2010 May;38(5):871-8.

    [4]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.

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