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

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEntecavirCat. No.: HY-13623CAS No.: 142217-69-4Synonyms: BMS200475; SQ34676分式: CHNO分量: 277.28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 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 44 mg/mL (158.68 mM)*

2、 means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.6065 mL 18.0323 mL 36.0646 mL5 mM 0.7213 mL 3.6065 mL 7.2129 mL10 mM 0.3606 mL 1.8032 mL 3.6065 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Entecavir（SQ 34676; BMS 200475）是有選擇且有效地HBV抑

3、制劑，在HepG2細(xì)胞中的EC50值為3.75 nM。IC50 & Target EC50: 3.75 nM (anti-HBV, HepG2 cell) 2體外研究BMS-200475 has a EC50 of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEsubsequently inhibits the priming step of the reverse transcriptase.

4、The antiviral activity of BMS-200475 issignificantly less against the other RNA and DNA viruses 1. Entecavir is more readily phosphorylated to itsactive metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) orlamivudine. The intracellular half-life of ent

5、ecavir is 15 h 2.體內(nèi)研究 Daily oral treatment with BMS-200475 at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1 to 3months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infectedwoodchucks 3.PROTOCOLCell Assay 1 BMS 200475 is prepared in phosphate-buf

6、fered saline (PBS) and diluted 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 w

7、ith BMS 200475. Quantification 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. Innai

8、mo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother.1997 Jul;41(7):1444-9.2. Rivkin A, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-57.3. 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):3209-18.McePdfHeightCaution: Product has not been fully validated for medical app