Dolutegravir, HIV integrase inhibitor (ab231511)

Overview

  • Product name

    Dolutegravir, HIV integrase inhibitor
  • Description

    Potent HIV integrase inhibitor
  • Alternative names

    • DTG
    • GSK1349572
    • S/GSK1349572
  • Biological description

    Potent HIV integrase inhibitor (IC50 = 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro). Inhibits HIV-1 viral replication (EC50 = 0.51 nM) in peripheral blood mononuclear cells (PBMCs). Prevents replication of several HIV-1 strains (EC50 values of 0.36-2.1 nM) that are resistant to nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), and protease inhibitors.

  • CAS Number

    1051375-16-6
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (4R,12aS)-N-[(2,4-Difluorophenyl)methyl]-7-hydroxy-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide

  • Molecular weight

    419.39
  • Molecular formula

    C20H19F2N3O5
  • PubChem identifier

    54726191
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • Solubility overview

    Soluble in DMSO to 5mM.

  • SMILES

    C[C@@H]1CCO[C@@H]2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
  • Source

    Synthetic

References

This product has been referenced in:

  • Kobayashi M  et al. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother 55:813-21 (2011). Read more (PubMed: 21115794) »
  • Hare S  et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol 80:565-72 (2011). Read more (PubMed: 21719464) »

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