Lopinavir (ABT-378), designed in response to Val82 mutant strains of HIV [1], is a potent inhibitor of HIV protease with Ki of 1.3-3.6 pM. Lopinavir inhibits replication of HIV-1 with an EC50 of 6-17 nM. [2]
Ritonavir was found to inhibit the metabolism of lopinavir with no other antagonistic effects; therefore lopinavir's drug exposure can be enhanced by co-formulation with ritonavir. In the presence of 50% human serum, the mean EC50 of lopinavir for five laboratory HIV-1 isolates ranged from 65 to 289 nM. [3]
Technical information:
| Chemical Formula: | C37H48N4O5 | |
| CAS #: | 192725-17-0 | |
| Molecular Weight: | 628.8 | |
| Purity: | > 98% | |
| Appearance: | White | |
| 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 | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | ABT-378, ABT378, Lopinavir |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Stoll et al., X-ray Crystallographic Structure of ABT-378 (Lopinavir) Boudn to HIV-1 Protease. Bioorg. Med. Chem. 2002, 10, 2803-2806. Pubmed ID: 12057670 |
| 2. | Sham et al., ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease. Antimicrob. Agents Chemother. 1998, 42(12), 3218-3224. Pubmed ID: 9835517 |
| 3. | Qazi et al., Lopinavir/ritonavir (ABT-378/r). Expert Opin. Pharmacother. 2002, 3(2), 315-327. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
