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Raltegravir potassium Chemical Structure

Raltegravir potassium

Data Sheet For research use only. Not for human use.
Cat. No. :BCP01757CAS No. :871038-72-1Purity:99%
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  • Chemical Properties&Biological Activity
CAS No. 871038-72-1 Cat. No. BCP01757
Name Raltegravir potassium
Synonyms MK-0518;Raltegravir Potassium Salt;Raltegravir;
SMILES
Chemical Name
Formula C20H20FKN6O5 M. Wt 444.41
Purity 99% Storage Store at 4-8°C
Description 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 is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31?0 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95 of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CY
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