Cat No.
CEI-0244
Description
Raltegravir (MK-0518, Isentress) can inhibit integrase(WT) and integrase (S217Q PFV) with IC50 of 90 nM and 40 nM.
Alias
Isentress
Synonyms
Isentress
CAS No.
518048-05-0
Targets
integrase(WT)
Chemical Name
N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(2-(2-methyl-1,3,4-oxadiazole-5-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide
M.Wt
444.42
Purity
>99%
Solubility
DMSO 89 mg/mL Water
Storage
2 years at -20centigrade Powder
In vitro
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.
In vivo
Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate shows an undetectable viral load following Raltegravir monotherapy.
