Dolutegravir-d3

CAT: 0804-HY-13238S1Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-13238S1Size:1 mg
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Description
Dolutegravir-d3 is the 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].
Product Name Alternative
S/GSK1349572-d3
UNSPSC
12352005
Target
HIV; HIV Integrase; Isotope-Labeled Compounds
Type
Isotope-Labeled Compounds
Related Pathways
Anti-infection; Metabolic Enzyme/Protease; Others
Field of Research
Infection
Purity
99.64
Solubility
10 mM in DMSO
Smiles
FC1=C([2H])C(F)=C(C=C1)C([2H])([2H])NC(C2=CN(C3=C(C2=O)O)C[C@@]([H])(N4C3=O)OCC[C@H]4C)=O
Molecular Formula
C20H16D3F2N3O5
Molecular Weight
422.40
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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