Lopinavir(ABT-378),designedinresponsetoVal82mutantstrainsofHIV[1],isapotentinhibitorofHIVproteasewithKiof1.3-3.6pM.LopinavirinhibitsreplicationofHIV-1withanEC50of6-17nM.[2]
RitonavirwasfoundtoinhibitthemetabolismoflopinavirwithnootherantagoNISTiceffects;thereforelopinavirsdrugexposurecanbeenhancedbyco-formulationwithritonavir.Inthepresenceof50%humanserum,themeanEC50oflopinavirforfivelaboratoryHIV-1isolatesrangedfrom65to289nM.[3]
Technicalinformation:
| ChemicalFormula: | C37H48N4O5 | |
| CAS#: | 192725-17-0 | |
| MolecularWeight: | 628.8 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | (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: | Upto100mMinDMSO | |
| Synonyms: | ABT-378,ABT378,Lopinavir |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Stolletal.,X-rayCrystallographicStructureofABT-378(Lopinavir)BoudntoHIV-1Protease.Bioorg.Med.Chem.2002,10,2803-2806.PubmedID:12057670 |
| 2. | Shametal.,ABT-378,aHighlyPotentInhibitoroftheHumanImmunodeficiencyVirusProtease.Antimicrob.AgentsChemother.1998,42(12),3218-3224.PubmedID:9835517 |
| 3. | Qazietal.,Lopinavir/ritonavir(ABT-378/r).ExpertOpin.Pharmacother.2002,3(2),315-327. |