HIV Protease Inhibitor
Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay.
Lopinavir 200mg
£966.00
Target: HIV protease (Cell-free assay) 1.3 pM(Ki)
Chemical name: (S)-N-((2S,4S,5S)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)-3-methyl-2-(2-oxo-tetrahydropyrimidin-1(2H)-yl)butanamide
Formula: C37H48N4O5
Molecular weight: 628.8
Purity: 99.92 %
Size: 200 mg
Solubility: 126 mg/mL (DMSO), 126 mg/mL (water)
Storage: 3 years -20°C powder, 2 years -80°C in solvent
In vitro:
Lopinavir binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. Lopinavir inhibits 93% of wild-type HIV protease activity at 0.5 nM. Lopinavir inhibits HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. [1] Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. [2] Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. [3] Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. [4] Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. [5]
In vivo:
Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. [1]
References:
[1] Sham HL, et al. Antimicrob Agents Chemother, 1998, 42(12), 3218-3224.
[2] Kumar GN, et al. Drug Metab Dispos, 1999, 27(1), 86-91.
[3] Vishnuvardhan D, et al. AIDS, 2003, 17(7), 1092-1094.
[4] Gonzalez LM, et al. Antimicrob Agents Chemother, 2003, 47(9), 2817-2822.
[5] Weemhoff JL, et al. J Pharm Pharmacol, 2003, 55(3), 381-386.