Tenofovir

N.º de catálogoS1401 Lote:S140104

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Datos técnicos

Fórmula

C9H14N5O4P
Peso molecular 287.21 Número CAS 147127-20-6
Solubilidad (25°C)* In vitro DMSO 5 mg/mL (17.4 mM)
Water 4 mg/mL (13.92 mM)
Ethanol Insoluble
In vivo (Agregue los solventes al producto individualmente y en orden.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción Tenofovir (GS-1278) bloquea la reverse transcriptase y las infecciones por el virus de la hepatitis B.
Objetivos
Reverse transcriptase
In vitro 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. This compound also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). It is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. This chemical inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. It (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. This compound inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 µM for wild-type RT, 6 µM for M184V RT and 50 µM for K65R RT.
In vivo Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. This compound reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. It completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques.
Características El fumarato de disoproxilo de tenofovir es la prodroga de tenofovir.

Protocolo (de referencia)

Estudio en animales:[1]
  • Modelos animales

    Macaques

  • Dosificaciones

    30 mg/kg

  • Administración

    Subcutaneously

Referencias

  • https://pubmed.ncbi.nlm.nih.gov/15040537/
  • https://pubmed.ncbi.nlm.nih.gov/11562951/
  • https://pubmed.ncbi.nlm.nih.gov/10760047/
  • https://pubmed.ncbi.nlm.nih.gov/10682153/
  • https://pubmed.ncbi.nlm.nih.gov/14557287/

Validación de productos por parte del cliente

<p>The Nucleotide analog reverse-transcriptase inhibitor Tenofovir disoproxil fumarate was added to TZM-bl cells. Cells were inoculated with 0.05 ng mock-exposed and semen-exposed HIV, and 0.5 ng HIV as infectivity-matched control. Infection rates were measured 3 days post infection by measuring β-galactosidase or or 4 days post infection by measuring luciferase activities. The left panels show the mean enzyme activities ± standard deviation derived from triplicate infections. RLU/s: relative light units per second. Middle panels show normalized infection rates in which reporter enzyme activities obtained from infected cells in the absence of inhibitor were set at 100%. The right panels depict the calculated IC50 values. The number above the bar represents the fold-change in the IC50 derived from 0.05 ng semen-exposed relative to 0.05 or 0.5 ng mock-exposed virus infection. Ns, no statistically significant difference; **** p<0.0001; *** p<0.001 (unpaired t-test).</p>

, , Sci Transl Med, 2014, 6(262):262ra157.

Selleck's Tenofovir Ha sido citado por 34 Publicaciones

LINE-1 ORF1p Mimics Viral Innate Immune Evasion Mechanisms in Pancreatic Ductal Adenocarcinoma [ Cancer Discov, 2025, 10.1158/2159-8290.CD-24-1317] PubMed: 39919290
Significance of hepatitis B virus capsid dephosphorylation via polymerase [ J Biomed Sci, 2024, 31(1):34] PubMed: 38561844
Nucleos(t)ide analogs for hepatitis B virus infection differentially regulate the growth factor signaling in hepatocytes [ Hepatol Commun, 2024, 8(1)e0351] PubMed: 38180972
Preclinical development of kinetin as a safe error-prone SARS-CoV-2 antiviral able to attenuate virus-induced inflammation [ Nat Commun, 2023, 14(1):199] PubMed: 36639383
Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223] PubMed: 37310224
The Development and Validation of RP-HPLC Method for Lamivudine, Dolutegravir, and Tenfovir in Human Plasma [ Pharm Res-Dordr, 2023, 21-40] PubMed: None
Understanding the role of NO-GC/cGMP in human, murine, and HIV-positive patients platelets and the effect of biochemical confinement in platelet morphology [ The Eberhard Karls University of Tübingen, 2023, ] PubMed: None
Understanding the role of NO-GC/cGMP in human, murine, and HIV-positive patient´ s platelets and the effect of biochemical confinement in platelet morphology and [ University of Tübingen, 2023, ] PubMed: NONE
Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021] PubMed: 35320348
Characterization of the tenofovir resistance-associated mutations in the hepatitis B virus isolates across genotypes A to D [ Antiviral Res, 2022, 203:105348] PubMed: 35644506

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