Name: Tenofovir Disoproxil Fumarate
Brand: Selleck Chemicals
SKU: S1400
Rating: 5 (28 reviews)

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Batch: Zuiverheid: 99.94%

99.94

Gerelateerde doelwitten	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease
Overig Reverse Transcriptase Inhibitoren	Dapivirine (TMC120) Fangchinoline Salicylanilide 3'-Fluoro-3'-deoxythymidine (Alovudine) Ulonivirine Lersivirine (UK-453061) Bifendate 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	635.51	Formule	C₁₉H₃₀N₅O₁₀P.C₄H₄O₄	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	202138-50-9	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid

In vitro
Batch:

DMSO : 100 mg/mL (157.35 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
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.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	5.000mg/ml (7.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.500mg/ml (3.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	HIV reverse transcriptase (Cell-free assay)
In vitro	Tenofovir wordt renaal uit de systemische circulatie geëlimineerd door een combinatie van glomerulaire filtratie en actieve tubulaire secretie. Tenofovir is geen substraat voor humane organische kationentransporter type 1 (hOCT1) of hOCT2. Tenofovir accumuleert tot vijf keer lagere niveaus in MRP4-overexpresserende cellen, en de accumulatie ervan zou kunnen worden verhoogd door een MRP-remmer. Tenofovir produceert geen significante veranderingen in mitochondriale DNA (mtDNA) niveaus in humane hepatoblastoom (HepG2) cellen, skeletspiercellen (SkMCs), of renale proximale tubulus epitheelcellen. Tenofovir verhoogt de lactaatproductie met minder dan 20% in HepG2 cellen of SkMCs. Tenofovir wordt efficiënt gefosforyleerd tot tenofovirdifosfaat (TFV-DP) in zowel HepG2 cellen als primaire humane hepatocyten. Tenofovir heeft een 50% effectieve concentratie van 1,1 mM tegen HBV in celgebaseerde assays, en de potentie wordt > 50-voudig verbeterd door de toevoeging van bis-isoproxil progroepen. Tenofovir heeft eerder volledige activiteit aangetoond tegen lamivudine-resistent HBV in vitro en klinisch. Tenofovir remt de proliferatie van lever-afkomstige HepG2 cellen en normale skeletspiercellen met CC(50) waarden van respectievelijk 398 μM en 870 μM. Tenofovir toont substantieel zwakkere effecten op de proliferatie en levensvatbaarheid van renale proximale tubulus epitheelcellen dan cidofovir, een verwant nucleotide-analoog met het potentieel om renale tubulaire disfunctie te induceren.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/17005808/ [2] https://pubmed.ncbi.nlm.nih.gov/11850253/ [3] https://pubmed.ncbi.nlm.nih.gov/16801428/ [4] https://pubmed.ncbi.nlm.nih.gov/11888656/ [5] https://pubmed.ncbi.nlm.nih.gov/26711762/ [6] https://pubmed.ncbi.nlm.nih.gov/25568137/

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT05874440	Recruiting	Chronic Hepatitis b Patients	Sohag University	April 15 2023	--
NCT03576066	Completed	Chronic Hepatitis B	Assembly Biosciences	June 11 2018	Phase 2
NCT03361956	Completed	Hepatitis B	Janssen Sciences Ireland UC	February 13 2018	Phase 2
NCT02985996	Completed	HIV Infections	Emory University\|Centers for Disease Control and Prevention	February 6 2017	Phase 1

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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Tenofovir Disoproxil Fumarate Reverse Transcriptase remmer

Chemische structuur

Molecuulgewicht: 635.51