Raltegravir-d6

Raltegravir-d6 is a deuterated labeled Raltegravir[1]. Raltegravir is a potent integrase (IN) inhibitor, used to treat HIV infection.

1100750-98-8

MK-0518-d6

12352005

HIV; HIV Integrase; Isotope-Labeled Compounds

Isotope-Labeled Compounds

Anti-infection; Metabolic Enzyme/Protease; Others

Infection

O=C(C1=NN=C(O1)C)NC(C)(C2=NC(C(NC([2H])([2H])C3=C([2H])C([2H])=C(C([2H])=C3[2H])F)=O)=C(C(N2C)=O)O)C

C20H15D6FN6O5

450.45

[1]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.|[2]Hare, S., et al., Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A, 2010. 107 (46) : p. 20057-62.|[3]Xu P, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12 (4) :682-692.|[4]Hicks C, et al. Raltegravir: the first HIV type 1 integrase inhibitor. Clin Infect Dis. 2009 Apr 1;48 (7) :931-9|[5]Lewis, M.G., et al. Response of a simian immunodeficiency virus (SIVmac251) to raltegravir: a basis for a new treatment for simian AIDS and an animal model for studying lentiviral persistence during antiretroviral therapy. Retrovirology, 2010. 7: p. 21.|[6]Moss DM, et al. Divalent metals and pH alter raltegravir disposition in vitro. Antimicrob Agents Chemother. 2012 Jun;56 (6) :3020-6|[7]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.

Room temperature

Isotope-Labeled Compounds