恩替卡韋 (1水合物)作用機制 - Medchemexpress - MCE中國

1、Product Data SheetEntecavir monohydrateCat. No.: HY-13623ACAS No.: 209216-23-9分式: CHNO分量: 295.29作靶點: HBV作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (169.33 mM)H2O : 2.8 mg/mL (9.48 mM; Need ultrasonic and warming)* means soluble,

2、 but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1

3、個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶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 solution此案可獲得 3 mg/mL (10.

4、16 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 30.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (10.16 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 3 mg/mL (10.16 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，

5、取 100 L 30.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3 mg/mL (10.16 mM); Clear solution此案可獲得 3 mg/mL (10.16 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 30.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Entecavir monohydr

6、ate (BMS200475 monohydrate; SQ34676 monohydrate)是有選擇且有效地HBV抑制劑。在HepG2細胞中的EC50值為3.75 nM。IC & Target EC50：3.75 nM (anti-HBV, HepG2 cell)1體外研究 Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) has a EC50 of 3.75 nM against HBV. It isincorporated into the protein primer of HBV and subse

7、quently inhibits the priming step of the reverse transcriptase.The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses1.Entecavir monohydrate is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs(penciclovir, ganciclovir,

8、lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h2.體內(nèi)研究 Daily oral treatment with Entecavir monohydrate 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 chronica

9、lly infected woodchucks3.PROTOCOLCell Assay 1 BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetalbovine serum. HepG2 2.2.15 cells are plated at a density of 5105 cells per well on 12-well Biocoat collagen-coatedplates and are maintained i

10、n a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked withBMS 200475. Quantification of HBV was performed on day 101.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 Mol Pharm. 2018 Oct 30. Virus Res. 2019 Jul 3

11、1:197677. bioRxiv. 2020 May.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCESPage 2 of 3 www.MedChemE1. Innaimo SF, et al. Identification of?BMS-200475?as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997Jul;41(7):1444-8.2. Rivkin A

12、, et al. A review of entecavir in the treatment of chronic hepatitis B infection. Curr Med Res Opin.?2005 Nov;21(11):1845-56.3. Genovesi EV, et al. Efficacy of the carbocyclic 2-deoxyguanosine nucleoside?BMS-200475?in the woodchuck model of hepatitis B virus infection.Antimicrob Agents Chemother.?1998 Dec;42(12):3209-17.McePdfHeightCaution: Product has not been