Amprenavir is a human immunodeficiency virus (HIV) protease inhibitor with IC50 of 14.6 ± 12.5 ng/ml for wild-type HIV isolates. Like all HIV protease inhibitors, amprenavir interrupts the maturation phase of the HIV replicative cycle by forming an inhibitor-enzyme complex, which prevents HIV protease from binding with its normal substrates. This compound has an enzyme inhibition constant (Ki = 0.6 nM) that falls within the Ki range of the other protease inhibitors. Amprenavir is an inhibitor of HIV-1 Protease.
Adkins, J.C., et al.: Drugs, 55, 837 (1998)
Soluble in DMSO (16 mg/ml at 25° C), chloroform, dichloromethane, ethanol (101 mg/ml at 25° C), and water (partly).
Rated 5 out of
DufekDufek, MB. et al. (PubMed 23821186) reported that intestinal first-pass metabolism by cytochrome p450 and not p-glycoprotein is the major barrier to Amprenavir absorption. -SCBT Publication Review
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