Raltegravir (MK-0518) - CAS 518048-05-0

Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.
PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM, indicating a ~twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme.
Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy.

Catalog Number: A000442

CAS Number: 518048-05-0

PubChem Substance ID:355039689

Molecular Formula: C20H21FN6O5

Molecular Weight:444.4

Purity: ≥95%

* For research use only. Not for human or veterinary use.

Synonym

SynonymsNA

Property

Molecular Formula: C20H21FN6O5
Molecular Weight444.4
Target:HIV Integrase
Solubility>20mg/mL in DMSO
Purity≥95%
Storage3 years -20C powder