Tenofovir-hydrate-GS-1278-hydrate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETenofovir hydrateCat. No.: HY-13910ACAS No.: 206184-49-8Synonyms: GS 1278 hydrate; PMPA hydrate; TDF hydrate分式: CHNOP分量: 305.23作靶點(diǎn): HIV; Reverse Transcriptase作通路: Anti-infection儲存式: 4C, stored under nitrogen* In solvent : -80C,

2、6 months; -20C, 1 month (stored undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 6 mg/mL (19.66 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.2762 mL 16.3811 mL 32.7622 mL5 mM 0.6552 mL 3.2762 mL 6.5524 mL10 mM 0.3276 mL 1.6381 mL 3.2762 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

3、，并請注意儲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)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?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；澄清的儲備液可以根據(jù)儲存條件，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: 0.6 mg/mL (1.97 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solub

4、ility: 0.6 mg/mL (1.97 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 0.6 mg/mL (1.97 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Tenofovir hydrate種于治療艾滋病毒和慢性型肝炎的核苷酸逆轉(zhuǎn)錄酶抑制劑。體外研究 Tenofovir shows cytotoxic effects on cell viability in H

5、K-2 cells, with IC50 values of 9.21 and 2.77 M at 48and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 M) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir inducesapoptosis in HK-2 cells, and that apopto

6、sis is induced via mitochondrial damage 1. Tenofovir and M48U1formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb inactivated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combinedformulation of M48U1 and t

7、enofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infectionwith R5-tropic HIV-1BaL, and is not toxic to PBMCs 2.體內(nèi)研究 Tenofovir Disoproxil Fumarate (20, 50, 140, or 300mg/kg) administered to BLT mice, shows dose dependentactivity during vaginal HIV challenge in BLT humanized

8、mice. Tenofovir Disoproxil Fumarate (50, 140, 300mg/kg) significantly reduces HIV transmission in BLT mice 3. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected withWHV. Tenofovir Disoproxil Fumarate ad

9、ministration is safe and effective in the woodchuck model of chronicHBV infection 4.PROTOCOLCell Assay 1 Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed bytreatment with vehicle or Tenofovir. Following the treatment period, cell viability i

10、s assessed using the MTTassay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only

11、.Animal Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serumAdministration 4 GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at15.0 mg/kg once per day, (ii) Tenofovir Disoproxil Fumarate at 5

12、.0 mg/kg/day, (iii) Tenofovir DisoproxilFumarate 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 daily for 4 weeks and observed for an additional 12 weeks following cessationof drug treatment 4.MCE has not independently conf

13、irmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Nanoscale. 2017 Jul 13;9(27):9676-9684. Sci Rep. 2017 Mar 15;7:44409.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Department od Analytical Chemistry, Charles University. 2019 Jun.See more customer validations on HYPERL

14、INK / www.MedChemEREFERENCES1. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar1;18(3).2. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and humancervicovag

15、inal histocultures. Sci Rep. 2017 Feb 1;7:41018.3. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic InVivo Model. Sci Rep. 2017 Feb 1;7:41098.4. Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronicwoodchuck hepatitis virus infection. Antimicrob Agents Che