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
Synonyms | NA |
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Property
Molecular Formula: | C20H21FN6O5 |
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Molecular Weight | 444.4 |
Target: | HIV Integrase |
Solubility | >20mg/mL in DMSO |
Purity | ≥95% |
Storage | 3 years -20C powder |