Raltegravir, HIV-1 integrase inhibitor (ab231360)

Overview

  • Product name

    Raltegravir, HIV-1 integrase inhibitor
  • Description

    Potent HIV-1 integrase inhibitor
  • Alternative names

    • Isentress
  • Biological description

    Raltegravir is a potent HIV-1 integrase inhibitor. It inhibits both wild-type and S217Q PFV integrase with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It is far less potent against the S217H PFV integrase mutant (IC50 = 900 nM). In cell-based assays Raltegravir inhibits HIV-1 with an IC95 of 31nM in human T lymphoid cells. It shows greater than 1000-fold selectivity for HIV-1 integrase compared to HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.

  • CAS Number

    518048-05-0
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide

  • Molecular weight

    444.42
  • Molecular formula

    C20H21FN6O5
  • PubChem identifier

    54671008
  • Storage instructions

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

    Soluble in DMSO to 198.01 mM.

  • Handling

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CC1=NN=C(O1)C(=O)NC(C)(C)C2=NC(=C(C(=O)N2C)O)C(=O)NCC3=CC=C(C=C3)F
  • Source

    Synthetic

References

This product has been referenced in:

  • 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) »
  • Hare S  et al. Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance. Proc Natl Acad Sci U S A 107:20057-62 (2010). Read more (PubMed: 21030679) »
  • Hicks C & Gulick RM Raltegravir: the first HIV type 1 integrase inhibitor. Clin Infect Dis 48:931-9 (2009). Read more (PubMed: 19231980) »

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