Dolutegravir-d3

• UNSPSC 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].

• Target Antigen:

  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 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)

• Clinical Information:

  No Development Reported