S/GSK1349572

S/GSK1349572

Catalog Number:
L002368994APE
Mfr. No.:
APE-A4074
Price:
$263
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      • Overview
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          Background

          S/GSK1349572, also known as dolutegravir, is a novel and potent inhibitor of human immunodeficiency virus (HIV) integrase (IN) blocking the strand transfer of integration of the viral genome into the host cell’s DNA. It occupies the physical space in the IN active site of the intasome, contacts with the β4-α2 loop of the catalytic core domain, and enters into the pocket vacated by the displaced viral DNA through its extended linker region connecting the metal chelating core the halobenzyl group. S/GSK1349572 exhibits potent anti-HIV activity in peripheral blood mononuclear cells (IC50 = 0.51 nM) in vitro and retains activity against raltegravir- and elvitegravir- resistant HIV.

      • Properties
        • Alternative Name
          S/GSK1349572, GSK-1349572; (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
          CAS Number
          1051375-16-6
          Molecular Formula
          C20H19F2N3O5
          Molecular Weight
          419.4
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          ≥41.9 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

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