Dolutegravir (sodium)

• Product Name Alternative:

  S/GSK1349572 (sodium)

• UNSPSC Description:

  Dolutegravir sodium (S/GSK1349572 sodium) 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 sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) 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

• Type:

  Reference compound

• Related Pathways:

  Anti-infection;Metabolic Enzyme/Protease

• Field of Research:

  Infection

• Assay Protocol:

  https://www.medchemexpress.com/Dolutegravir-sodium.html

• Purity:

  99.97

• Solubility:

  DMSO : 2 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : < 0.1 mg/mL (ultrasonic)

• Smiles:

  O=C(C1=CN(C2=C(O[Na])C1=O)C[C@]3([H])OCC[C@@H](C)N3C2=O)NCC4=CC=C(F)C=C4F

• Molecular Weight:

  441.36

• References & Citations:

  [1]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.|[2]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.|[3]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:

  4°C (Powder, sealed storage, away from moisture)

• Clinical Information:

  Launched

• CAS Number:

  1051375-19-9