Lopinavir

SKU: orb1307985

Description

Lopinavir (ABT-378) is a peptidomimetic inhibitor of HIV-1 protease that maintains efficacy against the Val82 mutant variant and exhibits reduced serum protein binding compared to ritonavir. It is widely used in antiviral research for in vitro enzyme assays and in vivo studies of HIV infection and resistance mechanisms.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

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Key Properties

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CAS Number	192725-17-0
MW	628.8
Purity	99.62%
Formula	C₃₇H₄₈N₄O₅
SMILES	[C@@H](C(N[C@@H](CC1=CC=CC=C1)C[C@@H]([C@H](CC2=CC=CC=C2)NC(COC3=C(C)C=CC=C3C)=O)O)=O)([C@@H](C)C)N4C(=O)NCCC4
Target	HIV Protease,SARS-CoV
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.36 mM);DMSO:247.5 mg/mL (393.61 mM);Ethanol:116 mg/mL (184.48 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	HIV protease:1.3 pM(Ki)
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. Read more...
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%.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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coadministration, ABT378, ABT-378, ABT 378, infection, inhibit, mutant, Lopinavir, Inhibitor, Human immunodeficiency virus, HIV protease, HIVProtease, HIV Protease, HIV, SARS-CoV, SARS coronavirus, SARSCoV, replication, wild-type

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Compound Identifiers

PubChem CID

92727 ↗

Key Properties

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No computed properties available.

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Lopinavir (orb1307985)

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CAS Number:	1322625-54-6
MW:	636.85
Formula:	C₃₇H₄₀D₈N₄O₅

CAS Number:	357275-54-8
MW:	644.8
Formula:	C₃₇H₄₈N₄O₆

MW:	756.92
Formula:	C₄₁H₄₈N₄O₈S

CAS Number:	192725-39-6
MW:	642.78
Formula:	C₃₇H₄₆N₄O₆

Purity:	>98%(HPLC)
CAS Number:	192725-17-0
MW:	628.8
Formula:	C₃₇H₄₈N₄O₅

Lopinavir

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Lopinavir (orb1307985)

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