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Tenofovir hydrate

Reverse transcriptase inhibitor CAS# 206184-49-8

Tenofovir hydrate

Catalog No. BCC4261----Order now to get a substantial discount!

Product Name & Size Price Stock
Tenofovir hydrate:5mg $71.00 In stock
Tenofovir hydrate:10mg $121.00 In stock
Tenofovir hydrate:25mg $284.00 In stock
Tenofovir hydrate:50mg $497.00 In stock
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Quality Control of Tenofovir hydrate

Quality Control & MSDS

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Chemical structure

Tenofovir hydrate

3D structure

Chemical Properties of Tenofovir hydrate

Cas No. 206184-49-8 SDF Download SDF
PubChem ID 21146529 Appearance Powder
Formula C9H16N5O5P M.Wt 305.23
Type of Compound N/A Storage Desiccate at -20°C
Synonyms GS 1278 hydrate; PMPA hydrate; TDF hydrate
Solubility DMSO : ≥ 6 mg/mL (19.66 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name [(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid;hydrate
SMILES CC(CN1C=NC2=C1N=CN=C2N)OCP(=O)(O)O.O
Standard InChIKey PINIEAOMWQJGBW-FYZOBXCZSA-N
Standard InChI InChI=1S/C9H14N5O4P.H2O/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14;/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17);1H2/t6-;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Tenofovir hydrate

DescriptionTenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.In Vitro:Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[1]. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs[2].In Vivo:Tenofovir Disoproxil Fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300 mg/kg) significantly reduces HIV transmission in BLT mice[3]. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection[4].

References:
[1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant 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;7:41018. [3]. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo 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 chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8.

Protocol

Cell Assay [1]
Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. 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].

Animal Administration [4]
Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once per day, (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 daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment[4].

References:
[1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant 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;7:41018. [3]. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo 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 chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8.

Tenofovir hydrate Dilution Calculator

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Tenofovir hydrate Molarity Calculator

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Preparing Stock Solutions of Tenofovir hydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.2762 mL 16.3811 mL 32.7622 mL 65.5244 mL 81.9054 mL
5 mM 0.6552 mL 3.2762 mL 6.5524 mL 13.1049 mL 16.3811 mL
10 mM 0.3276 mL 1.6381 mL 3.2762 mL 6.5524 mL 8.1905 mL
50 mM 0.0655 mL 0.3276 mL 0.6552 mL 1.3105 mL 1.6381 mL
100 mM 0.0328 mL 0.1638 mL 0.3276 mL 0.6552 mL 0.8191 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Tenofovir hydrate

Tenofovir hydrate is an inhibitor of reverse transcriptase used for the treatment of the human immunodeficiency virus 1(HIV-1) and hepatitis B [1].

Tenofovir hydrate is an antiviral pro-drug and the class of nucleoside reverse transcriptase inhibitor. In addition, Tenofovir hydrate has been reported to have a dependent relation between intracellular the drug concentrations and prevent function of HIV-1infection with EC50 values of 29 fmol/106, 40 fmol/106 , 77 fmol/106 and 411 fmol/106 cells for inoculum size 1, 5, 20 and 100 respectively. And the EC90 values of tenofovir hydrate are 267 fmol/106, 348 fmol/106, 640 fmol/106 and 2866 fmol/106 cells for virus inoculums size 1, 5, 20 and 100, respectively [1].

References:
[1] Duwal S1, Schütte C, von Kleist M.Pharmacokinetics and pharmacodynamics of the reverse transcriptase inhibitor tenofovir and prophylactic efficacy against HIV-1 infection. PLoS One. 2012;7(7):e40382. doi: 10.1371/journal.pone.0040382. Epub 2012 Jul 11.

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Description

Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

Keywords:

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