Molecular Formula | C29H43N3O8S
|
Molar Mass | 593.74 |
Melting Point | 98-100°C |
Solubility | Chloroform (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | White |
Storage Condition | Refrigerator |
Use | Darunavir Ethanolate is a human immunodeficiency virus (HIV) protease inhibitor. |
In vitro study | Darunavir shows potent activity against HIV strains that are resistant to other available protease inhibitors. In L- MDR1 cells, Darunavir(121 mM) inhibited P-glycoprotein-mediated efflux of calcein acetoxymethyl ester. Darunavir is a protein that inhibits phenylalanine sequences mimicking positions 167 and 168 of the GAG-POL polypeptide, binding to the active site of HIV protease, thereby inhibiting its activity. Darunavir inhibits infection and replication of HIV-1 variants at concentrations up to 5 μm. Darunavir showed strong antiretroviral activity against 19 recombinant clinical isolates carrying multiple protease mutations that showed resistance to the other five protien inhibitors. Darunavir inhibited 75% of the tested PI-resistant viruses with EC50 up to 10 nM. |
In vivo study | Darunavir is effective against wild-type and PI-resistant HIV, and has an oral bioavailability of 37%. It needs to be combined with ritonavir, which increases the bioavailability to 82%. |