Tenofovir maleate
Based on 10 publication(s) in Google Scholar
Tenofovir maleate (GS 1278 maleate; PMPA maleate) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).
For research use only. We do not sell to patients.
- CAS No.: 1236287-04-9
- Formula: C13H18N5O8P
- Molecular Weight:403.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Tenofovir maleate
More- Adv Sci (Weinh). 2022 Dec;9(34):e2203088. [Abstract]
- Nanoscale. 2017 Jul 13;9(27):9676-9684. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- Sci Rep. 2017 Mar 15:7:44409. [Abstract]
- Antiviral Res. 2020 Jun:178:104786. [Abstract]
- Pharm Res. 2023 Nov;40(11):2597-2606. [Abstract]
- Drug Metab Dispos. 2026 Mar 2;54(5):100263. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Dec 15:1267:124803. [Abstract]
- bioRxiv. 2025 Aug 14:2025.08.14.670267. [Abstract]
- Charles University. 2019 Jun.
Customer Validation & Images
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Bio/Physico-chemical Assay
Biological Activity
Description
IC50 & Target
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HIV-1 |
In Vitro
Tenofovir maleate displays cytotoxicity against HK-2 cells, with IC50 values of 9.21 μM at 48 h and 2.77 μM at 72 h determined by MTT assay. It reduces intracellular ATP levels, elevates oxidative stress and protein carbonylation, and triggers mitochondria-mediated apoptosis in HK-2 cells[1].
Tenofovir maleate formulated with M48U1 in 0.25% HEC inhibits the replication of R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and suppresses a panel of laboratory HIV-1 strains and patient-derived primary HIV-1 isolates. The combined formulation of Tenofovir maleate and M48U1 in 0.25% HEC delivers synergistic antiretroviral activity against R5-tropic HIV-1BaL infection and exhibits no cytotoxicity toward PBMCs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1236287-04-9
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Molecular Weight 403.28
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Formula C13H18N5O8P
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (10)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
SRSF5-Mediated Alternative Splicing of M Gene is Essential for Influenza A Virus Replication: A Host-Directed Target Against Influenza Virus. [Abstract]2022 Dec;9(34):e2203088. PMID: 36257906 -
Nanoscale
2017 Jul 13;9(27):9676-9684. PMID: 28675222 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Sci Rep
2017 Mar 15:7:44409. PMID: 28294122 -
Antiviral Res
Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro. [Abstract]2020 Jun:178:104786. PMID: 32251767 -
Pharm Res
Incorporating Uremic Solute-mediated Inhibition of OAT1/3 Improves PBPK Prediction of Tenofovir Renal and Systemic Disposition in Patients with Severe Kidney Disease. [Abstract]2023 Nov;40(11):2597-2606. PMID: 37704895
Tenofovir maleate purchased from MedChemExpress. Usage Cited in: Pharm Res. 2023 Nov;40(11):2597-2606. [Abstract]
Uremic solute inhibition of Tenofovir uptake. Human OAT1 and OAT3-overexpressing and mock-transfected HEK-293 cells were used for inhibition studies. Radiolabeled Tenofovir (0.1 μM) was added with potential inhibitors at specified concentrations for 5 min at 37 °C. Results of Tenofovir uptake were normalized to % of vehicle controls. IC50 shown in insets were calculated based on nonlinear regression curves.
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Drug Metab Dispos
A minimal physiologically based pharmacokinetic model for predicting the metabolism of tenofovir prodrugs in the liver of human with fibrosis. [Abstract]2026 Mar 2;54(5):100263. PMID: 42085925 -
J Chromatogr B Analyt Technol Biomed Life Sci
Development, validation and clinical implementation of a HPLC-MS/MS method for the simultaneous quantification of bictegravir, emtricitabine, doravirine, cabotegravir, lenacapavir, fostemsavir, tenofovir alafenamide and the corresponding metabolites temsavir and tenofovir, in human plasma. [Abstract]2025 Dec 15:1267:124803. PMID: 41072339 -
bioRxiv
Mechanistic insights and in vivo HIV suppression by the BRD4-targeting small molecule ZL0580. [Abstract]2025 Aug 14:2025.08.14.670267. PMID: 40832229 -
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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). [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tenofovir maleate Related Classifications
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