Entecavir-monohydrate-BMS200475-monohydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEntecavir monohydrateCat. No.: HY-13623ACAS No.: 209216-23-9Synonyms: BMS200475 (monohydrate); SQ34676 (monohydrate)分式: CHNO分量: 295.29作靶點(diǎn): HBV作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mo

2、nth溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (169.33 mM)H2O : 2.8 mg/mL (9.48 mM; Need ultrasonic and warming)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.3865 mL 16.9325 mL 33.8650 mL5 mM 0.6773 mL 3.3865 mL 6.7730 mL10 mM 0.3387 mL 1.6933 mL 3.3865 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度

3、，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的?chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (10.16 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in

4、saline)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 3 mg/mL (10.16 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3 mg/mL (10.16 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Entecavir monohydrate (BMS200475 monohydrate)是有選擇且有效地HBV抑制劑。在HepG2細(xì)胞中的EC50值為3.75 nM。IC50 & Tar

5、get EC50：3.75 nM (anti-HBV, HepG2 cell) 1體外研究 Entecavir monohydrate (BMS200475 monohydrate) has a EC50 of 3.75 nM against HBV. It is incorporatedinto the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. Theantiviral activity of BMS-200475 is significantl

6、y less against the other RNA and DNA viruses 1.Entecavir monohydrate is more readily phosphorylated to its active metabolites than other deoxyguanosineanalogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecaviris 15 h 2.體內(nèi)研究 Daily oral treatme

7、nt with Entecavir monohydrate at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1to 3 months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infectedwoodchucks 3.PROTOCOLCell Assay 1 BMS 200475 is prepared in phosphate-buffered saline (PBS) and dilute

8、d with appropriate medium containing2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5105 cells per well on 12-well Biocoatcollagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mLof medium spiked with BMS 200475. Quantificatio

9、n of HBV was performed on day 10 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Mol Pharm. 2018 Oct 30. Virus Res. 2019 Jul 31:197677.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Innaimo SF, et al. Identification

10、of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother.1997 Jul;41(7):1444-8.2. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. Genovesi EV, et al. Efficacy of the carbocyclic 2-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virusinfection. Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17.McePdfHeightCaution: Product has not been