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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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)

参考

  • https://pubmed.ncbi.nlm.nih.gov/12121928/
  • https://pubmed.ncbi.nlm.nih.gov/12665423/
  • https://pubmed.ncbi.nlm.nih.gov/18316521/
  • https://pubmed.ncbi.nlm.nih.gov/12878529/

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：

GDH1-dependent α-ketoglutarate promotes HBV transcription by modulating histone methylations on the cccDNA minichromosome [ Clin Mol Hepatol, 2025, 10.3350/cmh.2024.0694] PubMed: 39905842
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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。