Tenofovir maleate (Synonyms: GS 1278 maleate; PMPA maleate)

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

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No. CAS : 1236287-04-9

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Other In-stock Forms of Tenofovir maleate:

Tenofovir Tenofovir hydrate

Other Forms of Tenofovir maleate:

Tenofovir Disoproxil fumarate In-stock
Tenofovir In-stock
Tenofovir hydrate In-stock
Tenofovir diphosphate Obtener un presupuesto

10 Publications Citing Use of MCE Tenofovir maleate

Bio/Physico-chemical Assay

: 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. IC_{50_{shown in insets were calculated based on nonlinear regression curves.}}

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HIV HIV-1 HIV-2

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Descripciòn

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

IC₅₀ & Target

HIV-1

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-1_BaL and X4-tropic HIV-1_IIIb 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-1_BaL, and is not toxic to PBMCs^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Peso molecular

403.28

Fòrmula

C₁₃H₁₈N₅O₈P

No. CAS

1236287-04-9

SMILES

C[C@@H](OCP(O)(O)=O)CN1C=NC2=C(N)N=CN=C12.O=C(O)/C=C\C(O)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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]

Ensayo celular ^[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]. MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales ^[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]. MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias	[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]

Tenofovir maleate Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tenofovir1236287-04-9GS 1278PMPAGS1278GS-1278HIVReverse TranscriptaseHuman immunodeficiency virusInhibitorinhibitorinhibit

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