Nur für die Forschung bestimmt

Tenofovir Disoproxil Fumarate Reverse Transcriptase Inhibitor

Kat.-Nr.: S1400

Tenofovir Disoproxil Fumarate gehört zu einer Klasse von antiretroviralen Medikamenten. Es hemmt die Aktivität der HIV reverse transcriptase, indem es mit dem natürlichen Substrat Desoxyadenosin-5'-triphosphat konkurriert und, nach Einbau in die DNA, durch DNA-Kettenabbruch wirkt.
Tenofovir Disoproxil Fumarate Reverse Transcriptase Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 635.51

Springen zu

Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.94%
99.94

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
MT2 Function assay 5 days Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days, EC50=0.015μM 17562366
HepG2 Cytotoxicity assay 9 days Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=2.31μM 17888662
HepG2 Antiviral assay 9 days Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=5.1μM 17888662
MT-2 Antiviral assay Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, EC50=0.0068μM 19104010
MT2 Antiviral assay Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.54μM 19596885
HeLa P4/R5 Antiviral assay Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=4.7μM 19596885
HeLa P4/R5 Antiviral assay Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=11.4μM 19596885
human bone marrow cells Cytotoxicity assay 24 hrs Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=0.9μM 20439609
human bone marrow cells Cytotoxicity assay 24 hrs Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay, CC50=1.9μM 20439609
HeLa-T4 Antiviral assay 48 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC50=0.0029μM 21060108
HeLa-T4 Antiviral assay 48 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC95=0.037μM 21060108
HeLaT4 Antiviral assay 24 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi, EC50=0.12μM 21060108
HeLaT4 Antiviral assay Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated infection in human HeLaT4 cells treated for 1, EC99.6=0.95μM 21060108
HeLaT4 Cytotoxicity assay Cytotoxicity against human HeLaT4 cells by WST-1 assay, CC50=34μM 21060108
HeLaT4 Function assay 24 hrs Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs 21060108
HeLaT4 Antiviral assay 24 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed 21060108
PBMC Antiviral assay 7 days Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of viral replication by measuring reverse transcriptase activity in cell supernatant preincubated with cells followed by viral infection measured after 7 days by radioactive inc, EC50=0.0046μM 27405794
HepG2.2.15 Antiviral assay 3 days Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA in cell supernatant incubated for 3 days in presence of 10% FBS followed by compound treatment in absence of 10% FBS for 3 days by qRT-PCR method, EC50=0.34μM 27405794
HepG2.2.15 Cytotoxicity assay 6 days Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability after 6 days by XTT assay, CC50=29.2μM 27405794
PBMC Antiviral assay 30 mins Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured, IC50=0.08μM 28682067
PBMC Antiviral assay 30 mins Antiviral activity against CCR5 tropic HIV1 BaL infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured on , IC50=0.22μM 28682067
MT4 Antiviral assay 6 days Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 6 days by XTT dye based assay, EC50=4.89μM 28682067
MT4 Antiviral assay 6 days Antiviral activity against tenofovir-resistant CXCR4-tropic HIV-1 NL4-3 harboring reverse transcriptase K65R mutant infected in human MT4 cells assessed as inhibition of viral replication inhibition of virus-induced cytopathic effect after 6 days by XTT d, EC50=11.3μM 28682067
HepG2.2.15 Antiviral assay Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=0.85μM 31223460
HepG2.2.15 Cytotoxicity assay Cytotoxicity against human HepG2.2.15 cells infected with HBV, CC50=20.71μM 31223460
Klicken Sie hier, um weitere experimentelle Zellliniendaten anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 635.51 Formel

C19H30N5O10P.C4H4O4

Lagerung (Ab Erhaltdatum)
CAS-Nr. 202138-50-9 SDF herunterladen Lagerung von Stammlösungen

Synonyme GS 1278, Tenofovir DF Smiles CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 100 mg/mL (157.35 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewicht-Rechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie unten die Informationen ein (Empfohlen: Ein zusätzliches Tier einplanen, um Verluste während des Experiments auszugleichen)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, nicht die Formulierung. Bitte kontaktieren Sie uns zuerst, wenn im Abschnitt Löslichkeit keine In-vivo-Formulierung angegeben ist.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammflüssigkeit: mg Wirkstoff voraufgelöst in μL DMSO ( Konzentration der Stammflüssigkeit mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der jeweiligen Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzuμL PEG300, mischen und aufklären, fügen Sie als Nächstes hinzuμL Tween 80, mischen und aufklären, fügen Sie als Nächstes hinzu μL ddH2O, mischen und aufklären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzu μL Maisöl, mischen und aufklären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, die Lösungsmittel in der richtigen Reihenfolge hinzuzufügen. Sie müssen sicherstellen, dass die im vorherigen Schritt erhaltene Lösung klar ist, bevor Sie das nächste Lösungsmittel hinzufügen. Physikalische Methoden wie Vortexen, Ultraschall oder ein warmes Wasserbad können zur Unterstützung des Lösungsvorgangs verwendet werden.

Wirkungsmechanismus (Mechanism of Action)

Targets/IC50/Ki
HIV reverse transcriptase
(Cell-free assay)
In vitro

Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor. Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs. Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically. Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction.

Referenzen
  • [4] https://pubmed.ncbi.nlm.nih.gov/11888656/
  • [5] https://pubmed.ncbi.nlm.nih.gov/26711762/
  • [6] https://pubmed.ncbi.nlm.nih.gov/25568137/

Informationen zu klinischen Studien (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2026-08-14)

NCT-Nummer Rekrutierung Bedingungen Sponsor/Kollaboratoren Startdatum Phases
NCT07708727 RECRUITING
HIV-1-infection
Gilead Sciences
2026-07-29 PHASE2; PHASE3
NCT03304717 WITHDRAWN
Aicardi Goutières Syndrome
Children's Hospital of Philadelphia
2025-12 PHASE1; PHASE2
NCT07792096 NOT_YET_RECRUITING
HIV Infection
University College, London
2026-11 PHASE3
NCT06707922 ENROLLING_BY_INVITATION
Chronic Hepatitis B
Xiamen Amoytop Biotech Co., Ltd.
2022-03-18
NCT04375800 RECRUITING
Human Immunodeficiency Virus (HIV) Infection
Merck Sharp & Dohme LLC
2021-02-03 PHASE2
NCT07797231 NOT_YET_RECRUITING
Chronic Hepatitis B
Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
2026-09 PHASE3