Dolutegravir

• Description:

  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

• UNSPSC:

  12352005

• Hazard Statement:

  H400, H410

• Target:

  HIV; HIV Integrase

• Type:

  Reference compound

• Related Pathways:

  Anti-infection; Metabolic Enzyme/Protease

• Applications:

  COVID-19-anti-virus

• Field of Research:

  Infection

• Assay Protocol:

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

• Purity:

  99.85

• Solubility:

  DMSO : 35 mg/mL (ultrasonic)

• Smiles:

  FC1=CC(F)=C(C=C1)CNC(C2=CN(C3=C(C2=O)O)C[C@@]([H])(N4C3=O)OCC[C@H]4C)=O

• Molecular Formula:

  C20H19F2N3O5

• Molecular Weight:

  419.38

• Precautions:

  H400, H410

• 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:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  HIV-1

• Citation 01:

  Anal Bioanal Chem. 2018 Nov;410 (29) :7773-7781. |Antivir Ther. 2017;22 (8) :645-657. |Biochem Biophys Res Commun. 2017 Jul 1;488 (3) :433-438.|Biochem Pharmacol. 2024 Feb:220:116010.|bioRxiv. 2025 May 18.|Cell Physiol Biochem. 2016 Jul 21;39 (2) :639-650.|Cell Rep Med. 2024 Aug 26:101702.|Cell Rep Med. 2024 Jul 2:101643.|Cell. 2025 Sep 4;188 (18) :4896-4912.e19.|Drug Metab Dispos. 2019 Jul;47 (7) :768-778. |Drug Metab Dispos. 2019 May;47 (5) :535-544. |FASEB J. 2025 Feb 28;39 (4) :e70377.|Int J Antimicrob Agents. 2019 Dec;54 (6) :814-819.|J Clin Pharmacol. 2019 Sep;59 Suppl 1:S42-S55.|J Infect Dis. 2022 Nov 28;226 (11) :1992-2001.|J Neuroimmune Pharmacol. 2021 Mar;16 (1) :159-168.|Life Sci. 2022 Nov 1:308:120948.|Open Forum Infect Dis. 2024 Nov 29;12 (1) :ofae705.|PeerJ Physical Chemistry. 2019, 1:e6.|Pharmaceuticals (Basel) . 2022 Feb 18;15 (2) :242.|PLoS One. 2020 Jan 23;15 (1) :e0226924. |Preprints. 2024 Apr 23.|Res Sq. 2024 May 24.|Sci Adv. 2025 Sep 12;11 (37) :eadz8980. |Science. 2020 Feb 14;367 (6479) :806-810. |Toxicol Appl Pharmacol. 2019 Apr 1:368:18-25.|Viruses. 2021 Jan 18;13 (1) :131.|Viruses. 2024 Oct 13;16 (10) :1607.|Antiviral Res. 2025 Sep 11:106283.|Biomed Pharmacother. 2025 Nov 28:193:118831.

• CAS Number:

  1051375-16-6