Dolutegravir-d5(Synonyms: S/GSK1349572-d5)

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Dolutegravir-d5 (Synonyms: S/GSK1349572-d5)

Dolutegravir-d5 是 Dolutegravir 氘代物。Dolutegravir (S/GSK1349572) 是一种高效、口服的 HIV 整合酶链转移 抑制剂，在 HIV-1 整合酶催化的链转移中的 IC50 值为 2.7 nM，Dolutegravir (S/GSK1349572) 抑制 HIV-1 病毒在外周血单个核细胞中的复制，IC50 为 0.51 nM。Dolutegravir (S/GSK1349572) 对 Y143R，N155H 和 G140S/Q148H 突变体也保持高效 (EC50=3.6-5.8 nM)。

Dolutegravir-d5(Synonyms: S/GSK1349572-d5)

Dolutegravir-d5 Chemical Structure

CAS No. : 2249814-82-0

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生物活性

Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[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

424.41

Formula

C20H14D5F2N3O5
CAS 号

2249814-82-0
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]. Kobayashi M, et al. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.

    [3]. Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72.

    [4]. Moss L, et al. The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys. Xenobiotica. 2015 Jan;45(1):60-70.

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