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Tenofovir maleate (formerly also known as GS-1278; PMPA; TDF) is an approved anti-HIV drug that blocks reverse transcriptase and hepatitis B virus infections. Tenofovir is an antiretroviral medication used to prevent and treat HIV/AIDS and to treat chronic hepatitis B. Tenofovir reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). Tenofovir is the active substance of tenofovir disoproxil which is a prodrug that is used because of its better absorption in the gut.
| ln Vitro |
Tenofovir has a deleterious effect on the cell viability of HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 hours in MTT experiment, respectively. Tenofovir lowers ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) enhances oxidative stress and protein carbonylation in HK-2 cells. In addition, tenofovir can induce apoptosis in HK-2 cells, and apoptosis is triggered through mitochondrial damage [1]. Tenofovir and M48U1 formulated in 0.25% HEC both suppressed the replication of R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMC and inhibited several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC showed synergistic antiretroviral effectiveness against R5-tropic HIV-1BaL infection and was non-toxic to PBMC [2].
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| ln Vivo |
Tenofovir disoproxil fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice resulted in dose-dependent action in response to a vaginal HIV challenge in BLT humanized mice. HIV transmission in BLT mice is greatly decreased by tenofovir disoproxil fumarate (50, 140, and 300 mg/kg) [3]. In woodchucks with a chronic WHV infection, tenofovir disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day) causes a dose-dependent reduction in serum viremia. A woodchuck model of chronic HBV infection shows that tenofovir disoproxil fumarate is both safe and efficacious [4].
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| 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 |
| Molecular Formula |
C₁₃H₁₈N₅O₈P
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|---|---|
| Molecular Weight |
403.28
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| CAS # |
1236287-04-9
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| Related CAS # |
Tenofovir Disoproxil fumarate;202138-50-9;Tenofovir;147127-20-6;Tenofovir hydrate;206184-49-8;Tenofovir diphosphate;166403-66-3
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| SMILES |
C[C@@H](OCP(O)(O)=O)CN1C=NC2=C(N)N=CN=C12.O=C(O)/C=C\C(O)=O
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| Synonyms |
GS 1278 maleate PMPA maleate TDF maleateGS 1278 GS1278GS-1278PMPA TDF
GS1275 GS-1275 GS 1275 Tenofovir TFV gel PMPA
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4797 mL | 12.3983 mL | 24.7967 mL | |
| 5 mM | 0.4959 mL | 2.4797 mL | 4.9593 mL | |
| 10 mM | 0.2480 mL | 1.2398 mL | 2.4797 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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