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Lopinavir

Catalog No. T1623 CAS 192725-17-0

Synonyms: ABT-378

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.

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Lopinavir, CAS 192725-17-0

Pack Size	Availability	Price/USD
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

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Purity: 99.14%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 116 mg/mL (184.5 mM)

DMSO: 116 mg/mL (184.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Sham HL, et al. Antimicrob Agents Chemother, 1998, 42(12), 3218-3224. 2. Kumar GN, et al. Drug Metab Dispos, 1999, 27(1), 86-91. 3. Vishnuvardhan D, et al. AIDS, 2003, 17(7), 1092-1094. 4. Gonzalez LM, et al. Antimicrob Agents Chemother, 2003, 47(9), 2817-2822. 5. Weemhoff JL, et al. J Pharm Pharmacol, 2003, 55(3), 381-386. 6. Chu, Liuxi, et al. Simultaneous quantitation of zidovudine, efavirenz, lopinavir and ritonavir in human hair by liquid chromatography-atmospheric pressure chemical ionization-tandem mass spectrometry [J]. Journal of Chromatography B . 2018 Oct 15;1097-1098:54-63. 7. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123.

Citations

1. Cheng C, Ji Z, Sheng Y, et al. Aphthous ulcer drug inhibits prostate tumor metastasis by targeting IKKɛ/TBK1/NF-κB signaling. Theranostics. 2018, 8(17): 4633 2. Yan F, Gao F. An overview of potential inhibitors targeting non-structural proteins 3 (PLpro and Mac1) and 5 (3CLpro/Mpro) of SARS-CoV-2. Computational and Structural Biotechnology Journal. 2021, 19: 4868. 3. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library EMA Approved Drug Library Drug Repurposing Compound Library FDA-Approved & Pharmacopeia Drug Library FDA-Approved Drug Library Target-Focused Phenotypic Screening Library CNS-Penetrant Compound Library Human Metabolite Library ReFRAME Related Library Protease Inhibitor Library

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Keywords

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

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