Entecavir

Catalog No.S5246 Batch:S524601

Technical Data

Formula	C₁₂H₁₅N₅O₃
Molecular Weight	277.28	CAS No.	142217-69-4
Solubility (25°C)*	In vitro	DMSO	55 mg/mL (198.35 mM)
		Water	Insoluble
		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.)

Preparing Stock Solutions

Biological Activity

Description	Entecavir(BMS200475,SQ34676), a new deoxyguanine nucleoside analogue, is a selective inhibitor of the replication of the hepatitis B virus (HBV).
In vitro	For treatment of hepatitis B virus, combinations of ETV with each of the other HBV NRTI antivirals, adefovir, tenofovir, and lamivudine at 10 times their respective C^max levels fails to result in cellular or mitochondrial toxicity, and displays no DNA polymerase gamma inhibition.^[1]
In vivo	Treatment with Entecavir in combination with AIC649, Induces tightly regulated Immunological and virological responses during active and maintenance ereatment in the woodchuck model of chronic hepatitis B.

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HepG2 cells Concentrations 0.034 - 3.4 μM Incubation Time 15 days Method HepG2 cells (2.7 × 10₆) are seeded onto collagen I-coated T75 flasks. Cultures are exposed to compounds for a total of 15 days, reseeding every 5 days to the original cell density. In addition, media and compounds are also replaced 3 days after seeding. This schedule results in replacement of media containing fresh compound on days 1, 3, 5, 8, 10, and 13. Cells and culture supernatants are harvested and assayed on days 5, 10, and 15.

Cell Assay:^{^[1]}

Cell lines
HepG2 cells
Concentrations
0.034 - 3.4 μM
Incubation Time
15 days
Method
HepG2 cells (2.7 × 10₆) are seeded onto collagen I-coated T75 flasks. Cultures are exposed to compounds for a total of 15 days, reseeding every 5 days to the original cell density. In addition, media and compounds are also replaced 3 days after seeding. This schedule results in replacement of media containing fresh compound on days 1, 3, 5, 8, 10, and 13. Cells and culture supernatants are harvested and assayed on days 5, 10, and 15.

References

[1] Mazzucco CE, et al. Antimicrob Agents Chemother. 2008 Feb;52(2):598-605.

Selleck's Entecavir has been cited by 13 publications

A therapeutic hepatitis B mRNA vaccine with strong immunogenicity and persistent virological suppression [ NPJ Vaccines, 2024, 9(1):22]	PubMed: 38310094
Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021]	PubMed: 35320348
In vitro investigation of HBV clinical isolates from Chinese patients reveals that genotype C isolates possess higher infectivity than genotype B isolates [ Virol Sin, 2022, S1995-820X(22)00062-1]	PubMed: 35314401
Rapamycin inhibits hepatitis B virus covalently closed circular DNA transcription by enhancing the ubiquitination of HBx [ Front Microbiol, 2022, 13:850087]	PubMed: 36033851
Genotoxicity assessment of potentially mutagenic nucleoside analogues using ToxTracker® [ Toxicol Lett, 2022, 362:50-58]	PubMed: 35569722
Preclinical characterization of AB-506, an inhibitor of HBV replication targeting the viral core protein [ Antiviral Res, 2021, 197:105211]	PubMed: 34826506
A cell-based assay to discover inhibitors of SARS-CoV-2 RNA dependent RNA polymerase [ Antiviral Res, 2021, S0166-3542(21)00068-1]	PubMed: 33894278
Treatment with the Immunomodulator AIC649 in Combination with Entecavir Produces Antiviral Efficacy in the Woodchuck Model of Chronic Hepatitis B [ Viruses, 2021, 13(4)648]	PubMed: 33918831
Anti-HBV therapeutic potential of small molecule 3,5,6,7,3',4'-Hexamethoxyflavone in vitro and in vivo [ Virology, 2021, 560:66-75]	PubMed: 34051476
HBV Core Promoter Inhibition by Tubulin Polymerization Inhibitor (SRI-32007) [ Adv Virol, 2020, 2020:8844061]	PubMed: 33110426

RETURN POLICY
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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.

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