Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor that retains activity against HIV protease with the Val 82 mutation. Lopinavir is less affected by binding to serum proteins than the structurally-related drug ritonavir.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
50 mg | In stock | $ 41.00 | |
100 mg | In stock | $ 66.00 | |
200 mg | In stock | $ 97.00 | |
500 mg | In stock | $ 198.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 45.00 |
Description | Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor that retains activity against HIV protease with the Val 82 mutation. Lopinavir is less affected by binding to serum proteins than the structurally-related drug ritonavir. |
Targets&IC50 | HIV protease:1.3 pM(Ki) |
In vitro | Administering Lopinavir (10 mg/kg, p.o.) to rats resulted in a maximum concentration (Cmax) of 0.8 μg/mL, with the drug's bioavailability being 25%. |
In vivo | Lopinavir is an effective inhibitor of Rh123, with an IC50 value of 1.7 mM for Caco-2 cell monolayers. It binds to mutant HIV proteases (V82A, V82T, and V82F) with Ki values of 4.9, 3.7, and 3.6 pM, respectively. At a concentration of 0.5 nM, Lopinavir inhibits the activity of wild-type HIV protease by 93%. It also inhibits HIV protease activity in MT4 cells both in the presence and absence of 50% HS, with EC50 values of 102 nM and 17 nM, respectively. In liver microsomes, Lopinavir is converted to primary metabolites M-3 and M-4, a process that is NADPH-dependent. After treating LS 180V cells with Lopinavir for 72 hours, there is a reduction in intracellular Rh123 content and induction of P-glycoprotein immunoreactive protein and mRNA levels. Lopinavir exhibits an IC50 of 9.4 nM against subtype C clone C6. When acting on human liver microsomes, Lopinavir shows an IC50 of 7.3 mM against CYP3A and exerts weak inhibition on human CYP1A2, 2B6, 2C9, 2C19, and 2D6. |
Synonyms | ABT-378 |
Molecular Weight | 628.8 |
Formula | C37H48N4O5 |
CAS No. | 192725-17-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 116 mg/mL (184.5 mM)
DMSO: 116 mg/mL (184.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Lopinavir 192725-17-0 Microbiology/Virology Proteases/Proteasome SARS-CoV HIV Protease ABT-378 inhibit coadministration SARS coronavirus mutant Inhibitor wild-type HIV Human immunodeficiency virus infection ABT378 replication ABT 378 inhibitor