Entecavir Hydrate

Catalog No.S1252 Batch:S125201

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Technical Data

Formula

C12H15N5O3.H2O

Molecular Weight 295.29 CAS No. 209216-23-9
Solubility (25°C)* In vitro DMSO 59 mg/mL (199.8 mM)
Ethanol 2 mg/mL (6.77 mM)
Water 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 Entecavir Hydrate (ETV, Baraclude,BMS200475 Hydrate,SQ34676 Hydrate), a new deoxyguanine nucleoside analogue, is a selective inhibitor of the replication of the hepatitis B virus (HBV).
Targets
Reverse Transcriptase [1]
In vitro

Entecavir-triphosphate is a highly potent inhibitor of wild-type HBV Pol and is 100- to 300-fold more potent than lamivudine-triphosphate against 3TC-resistant HBV Pol. Entecavir inhibits the replication of 3TC-resistant HBV, but 20- to 30-fold higher concentrations are required. [1] Entecavir results in an impressive reduction of serum viral DNA with covalently closed circular DNA and hepatitis B viral core antigen negativity in liver biopsy specimens. [2] Entecavir has potent activity (EC50, 0.1 nM) against HIV in a unique single-cycle, single-cell-based pseudovirus assay (24) with CD4+ lymphocytes using a green fluorescent protein reporter fluorescence-activated cell sorter assay as the endpoint. [3]

In vivo

Entecavir causes a 4-log drop in serum DHBV DNA levels within 80 days and a slower 2- to 3-log drop in serum DHBV surface antigen (DHBsAg) levels within 120 days in ducks. Entecavir treatment reduces DHBV DNA replicative intermediates 70-fold in the liver, while the level of the stable, template form, covalently closed circular DNA decreases only 4-fold in ducks. Entecavir treatment reduces both the intensity of antigen staining and the percentage of antigen-positive hepatocytes in the liver, but the intensity of antigen staining in bile duct cells appeares not to be effected in ducks. [4]

Protocol (from reference)

Selleck's Entecavir Hydrate has been cited by 11 publications

Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021] PubMed: 35320348
Alpha-kinase 1 (ALPK1) agonist DF-006 demonstrates potent efficacy in mouse and primary human hepatocyte (PHH) models of hepatitis B [ Hepatology, 2022, 10.1002/hep.32614] PubMed: 35699669
Drug screen in iPSC-Neurons identifies nucleoside analogs as inhibitors of (G4C2)n expression in C9orf72 ALS/FTD [ Cell Rep, 2022, 39(10):110913] PubMed: 35675776
Coinfection of Clonorchis sinensis and hepatitis B virus: clinical liver indices and interaction in hepatic cell models [ Parasit Vectors, 2022, 15(1):460] PubMed: 36510325
Coinfection of Clonorchis sinensis and hepatitis B virus: clinical liver indices and interaction in hepatic cell models [ Parasit Vectors, 2022, 15(1):460] PubMed: 36510325
SARS-CoV-2 RdRp Inhibitors Selected from a Cell-Based SARS-CoV-2 RdRp Activity Assay System [ Biomedicines, 2021, 9(8)996] PubMed: 34440200
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
Interferon alpha antagonizes the anti-hepatoma activity of the oncolytic virus M1 by stimulating anti-viral immunity. [ Oncotarget, 2017, 8(15):24694-24705] PubMed: 28445966

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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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