Entecavir Hydrate

製品コードS1252 バッチS125203

印刷

化学情報

Chemical Structure Synonyms ETV, Baraclude,BMS200475 Hydrate,SQ34676 Hydrate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H15N5O3.H2O
分子量 295.29 CAS No. 209216-23-9
Solubility (25°C)* 体外 DMSO 59 mg/mL (199.8 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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).
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]

プロトコル(参考用のみ)

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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