Ledipasvir-d6(Synonyms: GS-5885-d6)

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Ledipasvir-d6 (Synonyms: GS-5885-d6)

Ledipasvir-d6 (GS-5885-d6) 是 Ledipasvir 的氘代物。Ledipasvir (GS-5885) 是一种有效的 HCV NS5A 抑制剂，能够抑制 GT1a 和 GT1b 复制子，EC50 值分别为 34 pM 和 4 pM。Ledipasvir 也是 SARS-CoV 3CLpro 的抑制剂，IC50 为 1.62 μM。

Ledipasvir-d6(Synonyms: GS-5885-d6)

Ledipasvir-d6 Chemical Structure

CAS No. : 2050041-12-6

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生物活性

Ledipasvir-d6 (GS-5885-d6) is the deuterium labeled Ledipasvir. Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. Ledipasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM[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

895.04

Formula

C49H48D6F2N8O6
CAS 号

2050041-12-6
中文名称

雷迪帕韦 d6
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]. Link JO, et al. Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection. J Med Chem. 2014 Mar 13;57(5):2033-46

    [3]. Hernandez D, et al. Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effects on the antiviral activity of NS5A inhibitors. J Clin Virol. 2013 May;57(1):13-8.

    [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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