【产品介绍】：

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].
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Dolutegravir-d5 相关抗体:
CD4 Antibody
TARBP2 Antibody (YA1433)
SAMHD1 Antibody (YA1542)
SV40 T Antigen Antibody (YA3256)
CLEC12A Antibody (YA1419)
Tat SF1 Antibody (YA2886)
分子量：424.41
Formula：C20H14D5F2N3O5
CAS 号：2249814-82-0
非标记 CAS：1051375-16-6
中文名称：度鲁特韦-d5；德罗特韦-d5
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.
纯度 & 产品资料
Data Sheet (533 KB)
产品使用指南 (1538 KB)
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.
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[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.
 [Content Brief]
[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.
 [Content Brief]
[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.
 [Content Brief]