HIV protease inhibitor
Darunavir Ethanolate (DRV) is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
Darunavir Ethanolate 50 mg
£966.00
Target: HIV protease
Chemical name: N-[(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl carbamic acid ester, compd. with ethanol (1:1)
Formula: C27H37N3O7S.C2H5OH
Molecular weight: 593.73
Size: 50 mg
Purity: 99.88 %
Solubility: 100 mg/mL (DMSO)
Storage: 3 years -20°C powder, 2 years -80°C in solvent
In vitro:
Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM. Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM.