| Agenerase is a highly stereoselective synthesis of the HIV protease inhibitor. The IC50 of agenerase ranges from 2.5 to 2.9 μM against HIV proteases. Pre-incubation of microsomes with agenerase increases inhibitory potency with an IC50 of 1.4μM.[1]Agenerase blocks the catalytic activity of XMRV protease.[2] Agenerase has 2-to 23-fold higher transport rates from the basolateral to apical direction than from the apical to basolateral direction across Caco-2 monolayers.[3] Agenerase is highly bound to human plasma proteins (～90%). Agenerase primarily binds to α1-acid glycoprotein (AAG) and albumin, with fractional binding of 89 and 42%, respectively.[4] The clearance index of agenerase is 0.38 and 0.14 at peak and trough concentrations, respectively.[5] Agenerase metabolism in rat liver microsomes is strongly inhibited by indinavir.[6] |
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