HIV protease inhibitor
Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
Nelfinavir Mesylate (200mg)
£973.00
SKU: BSV-S4282-200
Target: HIV protease (Cell-free assay) 2nM
Chemical name: N-(1,1-dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-(3S,4aS,8aS)-3-isoquinolinecarboxamide, methanesulfonate (1:1)
Formula: C33H49N3O7S2
Molecular weight: 663.89
Purity: 99.43 %
Solubility: 100 mg/mL (DMSO), 100 mg/mL (ethanol)
Size: 200 mg
Storage: 3 years -20°C powder, 2 years -80°C in solvent
In vivo:
In vivo studies indicate that AG1343 is well absorbed orally in a variety of species and possesses favorable pharmacokinetic properties in humans. Initial investigation of the compound in fed rats indicated an oral bioavailability of 43%. In contrast, the oral bioavailability was significantly reduced in fasted rats to 29%. Nelfinavir demonstrated significant oral bioavailabilability across a range of species including dogs (47%), marmosets (17%), and cynomolgus monkeys (26%). It has a long plasma half-life after oral dosing that is likely due to a combination of slow dissolution and absorption. nelfinavir is well absorbed in humans particularly when administered with food and possesses minimal and easily managed side effects[1].
References:
[1] Kaldor SW, et al.J Med Chem, 1997,40(24):3979-85.