Tenofovir maleateReverse transcriptase inhibitor CAS# 1236287-04-9 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1236287-04-9 | SDF | Download SDF |
| PubChem ID | 53302693 | Appearance | Powder |
| Formula | C13H18N5O8P | M.Wt | 403.28 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | GS 1278 maleate; PMPA maleate; TDF maleate | ||
| Solubility | Soluble in DMSO | ||
| Chemical Name | [(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid;(Z)-but-2-enedioic acid | ||
| SMILES | CC(CN1C=NC2=C1N=CN=C2N)OCP(=O)(O)O.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | OPQKUDVCYGLXAH-REVJHSINSA-N | ||
| Standard InChI | InChI=1S/C9H14N5O4P.C4H4O4/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14;5-3(6)1-2-4(7)8/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17);1-2H,(H,5,6)(H,7,8)/b;2-1-/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. |
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| 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. |
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| 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. | ||
| Description | Tenofovir Disoproxil Fumarate 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: | |||||
Tenofovir maleate Dilution Calculator
Tenofovir maleate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4797 mL | 12.3983 mL | 24.7967 mL | 49.5933 mL | 61.9917 mL |
| 5 mM | 0.4959 mL | 2.4797 mL | 4.9593 mL | 9.9187 mL | 12.3983 mL |
| 10 mM | 0.248 mL | 1.2398 mL | 2.4797 mL | 4.9593 mL | 6.1992 mL |
| 50 mM | 0.0496 mL | 0.248 mL | 0.4959 mL | 0.9919 mL | 1.2398 mL |
| 100 mM | 0.0248 mL | 0.124 mL | 0.248 mL | 0.4959 mL | 0.6199 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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Tenofovir maleate is an inhibitor of reverse transcriptase used for the treatment of the human immunodeficiency virus 1(HIV-1) and hepatitis B [1].
Tenofovir maleate is an antiviral pro-drug and the class of nucleoside reverse transcriptase inhibitor. In addition, Tenofovir maleate 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 EC50 values of tenofovir maleate 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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