Lamivudine

Catalog No.S1706 Batch:S170602

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Technical Data

Formula

C8H11N3O3S

Molecular Weight 229.26 CAS No. 134678-17-4
Solubility (25°C)* In vitro DMSO 45 mg/mL (196.28 mM)
Water 45 mg/mL (196.28 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor, used for treatment of chronic HBV and HIV/AIDS. It works by blocking the HIV reverse transcriptase and hepatitis B virus polymerase.
Targets
Reverse transcriptase [1]
In vitro

Lamivudine’s anti- HBV activity, like its anti-HIV activity, has been shown to depend on the ability of LMV-TP to serve as both substrate and inhibitor of the DNA- and RNA-dependent polymerase activities of the HBV P gene product. Lamivudine owes its activity to the remarkably broad substrate specificity of deoxycytidine kinase and the unusual substrate preference of the HBV polymerases for dNTPs with the unnatural L-conformation, whereas the anti-HBV activity of PCV appears to depend on several factors including optimal phosphorylation (sufficient for antiviral activity but not cytotoxicity) by key cellular enzymes, the long intracellular half-life of PCV-TP and the ability of PCV-TP to inhibit the HBV RT priming reaction as well as RT and DNA polymerase activity. [1]

Lamivudine and Penciclovir inhibits duck hepatitis B virus (DHBV) replication to a comparable extent when used alone, and in combination, the two nucleoside analogs acts synergistically over a wide range of clinically relevant concentrations. Lamivudine combined with Penciclovir is more effective in reducing the normally recalcitrant viral covalently closed circular (CCC) DNA form of DHBV than either drug alone. [2]

Lamivudine inhibits p24 antigen production by HIV-I in PBMC, with ED50s ranging from 0.07 μM to 0.2 μM. [3]

Protocol (from reference)

Cell Assay:

[4]

  • Cell lines

    Neonatal rat ventricular cardiomyocytes

  • Concentrations

    5 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentrations of drug for 24 h.

Customer Product Validation

Data from [Data independently produced by , , Oncotarget, 2017, 8(15):24694-24705]

Selleck's Lamivudine has been cited by 16 publications

Screening of an epigenetic compound library identifies BRD4 as a potential antiviral target for hepatitis B virus covalently closed circular DNA transcription [ Antiviral Res, 2023, 211:105552] PubMed: 36737008
Farnesoid X receptor alpha ligands inhibit HDV in vitro replication and virion infectivity [ Hepatol Commun, 2023, 7(5)e0078] PubMed: 37058078
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] PubMed: 37310224
Kamuvudine-9 Protects Retinal Structure and Function in a Novel Model of Experimental Rhegmatogenous Retinal Detachment [ Invest Ophthalmol Vis Sci, 2023, 64(5):3] PubMed: 37129905
Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021] PubMed: 35320348
Hepatitis B virus X protein counteracts high mobility group box 1 protein-mediated epigenetic silencing of covalently closed circular DNA [ PLoS Pathog, 2022, 18(6):e1010576] PubMed: 35679251
Reduction of CD8 T cell functionality but not inhibitory capacity by integrase inhibitors [ J Virol, 2022, JVI0173021] PubMed: 35019724
Antiretroviral Drugs Regulate Epigenetic Modification of Cardiac Cells Through Modulation of H3K9 and H3K27 Acetylation [ Front Cardiovasc Med, 2021, 8:634774] PubMed: 33898535
Identification and characterization of a novel hepatitis B virus pregenomic RNA encapsidation inhibitor. [ Antiviral Res, 2020, 175:104709] PubMed: 31940474
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536] PubMed: 33346662

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.