1、Product Data SheetTenofovir DisoproxilCat. No.: HY-13782ACAS No.: 201341-05-1分式: CHNOP分量: 519.44作靶點(diǎn): HIV; Reverse Transcriptase; 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 : 38 mg/mL (73.16 mM)* means soluble, but saturation unknown.Sol

2、ventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 1.9252 mL 9.6258 mL 19.2515 mL5 mM 0.3850 mL 1.9252 mL 3.8503 mL10 mM 0.1925 mL 0.9626 mL 1.9252 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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙?/p>

3、案。以下溶解案都請(qǐng)先按照 In Vitro 式配制澄清的儲(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，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.00 mM); Clear solution此案可獲得 2.08 mg/mL (4.00 mM，飽和度未知) 的澄清溶液。以 1 m

4、L 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.00 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.08 mg/mL (4.00 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的

5、澄 DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.00 mM); Clear solution此案可獲得 2.08 mg/mL (4.00 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Tenofovir Disoproxil (Bis(POC)-PMP

6、A)療艾滋病和慢性型肝炎。核苷酸逆轉(zhuǎn)錄酶抑制劑 (nucleotide reverse transcriptase inhibitor)，于治體外研究 Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 M at 48 and 72 h inMTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 M) increa

7、ses oxidativestress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and thatapoptosis is induced via mitochondrial damage1. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits thereplication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in

8、activated PBMCs, and inhibits several laboratorystrains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibitssynergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs2.體內(nèi)研究 Tenofovir Disoproxil Fumarat

9、e (20, 50, 140, or 300 mg/kg) administered to BLT mice, shows dose dependent activityduring vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300 mg/kg) significantlyreduces HIV transmission in BLT mice3. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p

10、.o.) induces adose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir DisoproxilFumarate administration is safe and effective in the woodchuck model of chronic HBV infection4.PROTOCOLCell Assay 1 Cells are plated into 48-well tissue culture plates (39,000 cells

11、/mL) and allowed to grow for 48 h followed bytreatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. TheMTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide(MTT) to formazan by N

12、AD(P)H-dependent oxidoreductases.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activityAdministration 4 into five treatment groups consis

13、ting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once perday, (ii) Tenofovir Disoproxil Fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5 mg/kg/day, (iv)Tenofovir Disoproxil Fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated

14、 daily for 4weeks and observed for an additional 12 weeks following cessation of drug treatment.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)Page 2 of 3 www.MedChemE Int J Antimicrob Agents. 2019 Dec;54(6):814-819. Sci Rep. 2019 Nov 20;9(1

15、):17158. J Neuroimmune Pharmacol. 2019 Jul 23. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. Department od Analytical Chemistry, Charles University. 2019 Jun.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Murphy RA, et al. Establishment of HK-2 Cells as a Relevan

16、t Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3)2. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures.Sci Rep. 2017 Feb 1;7:410183. Wahl A, et al. Predicting HIV Pre-expos

17、ure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep.2017 Feb 1;7:410984. Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virusinfection. Antimicrob Agent