Cat. No. Name Size Price Add Cart
KI1287Lopinavir10 mg$130
Lopinavir100 mg$550
Lopinavir200 mg$990

Chemical Characteristic

Product NameLopinavir
SynonymsABT-378
CAS No.192725-17-0
Molecular Weight 628.81
FormulaC37H48N4O5
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
SmilesC(=O)([C@H](C(C)C)N1C(=O)NCCC1)NC(Cc1ccccc1)C[C@@H]([C@H](Cc1ccccc1)NC(=O)COc1c(cccc1C)C)O
Chemical Structure

Biological activities

Lopinavir is a potent HIV protease inhibitor. The Ki of lopinavir is 1.3 pM against wild-type HIV protease.[1]Lopinavir (LPV) is a second-generation HIV protease inhibitor designed to used in the long-term antiviral therapy.[2]On the other hand, lopinavir inhibits mutant HIV proteaseV82A mutant HIV proteaseV82F, mutant HIV proteaseV82T with Ki of 4.9, 3.7 and 3.6pM, respectively. Lopinavir blocks the replication of isolated strains of HIV type 1 with an EC50 ranging from 6 to 17 nM. Lopinavir keeps high potency against mutant HIV in vivo with an EC50 of 60 nM.[1]Lopinaviris metabolized very extensively and rapidly by liver microsomes from mouse, rat, dog, monkey, and humans. The rates of NADPH-dependent metabolism of lopinavir ranges from 2.39 to 9.80 nmol/mg microsomal protein/minute, with monkey liver microsomes exhibiting the highest rates of metabolism.[3]When administered at a dose of 400 mg of lopinavirand 100 mg of ritonavir twice daily, the resultingmean trough lopinavir concentrations are at least 75times as high as the protein binding-corrected con-centration needed to inhibit the replication of wild-type HIV by 50 percent.[4]

Protocols

In vitro: Lopinaviris dissolved in DMSO.[2]

References

[1]Sham HL, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease.Antimicrob Agents Chemother. 1998, 42(12):3218-3224.
[2]Saskov? KG, et al. Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir.Protein Sci. 2008, 17(9): 1555-1564.
[3]Kumar GN, et al. In vitro metabolism of the HIV-1 protease inhibitor ABT-378: species comparison and metabolite identification.Drug MetabDispos. 1999, 27(1):86-91.
[4] Walmsley S, et al. Lopinavir-ritonavir versus nelfinavir for the initial treatment of HIV infection.N Engl J Med. 2002, 346(26):2039-2046.

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