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

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Control de calidad

Lote: Pureza: 99.94%

99.94

Dianas relacionadas	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease
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Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Tiempo de incubación	Descripción de la actividad	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
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Información química, almacenamiento y estabilidad

Peso molecular	635.51	Fórmula	C₁₉H₃₀N₅O₁₀P.C₄H₄O₄	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	202138-50-9	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	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

Solubilidad

In vitro
Lote:

DMSO : 100 mg/mL (157.35 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 100 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Targets/IC₅₀/Ki	HIV reverse transcriptase (Cell-free assay)
In vitro	El tenofovir se elimina de la circulación sistémica por vía renal a través de una combinación de filtración glomerular y secreción tubular activa. El tenofovir no es un sustrato para el transportador de cationes orgánicos humanos tipo 1 (hOCT1) o hOCT2. El tenofovir se acumula a niveles cinco veces menores en las células que sobreexpresan MRP4, y su acumulación podría aumentar con un inhibidor de MRP. El tenofovir no produce cambios significativos en los niveles de ADN mitocondrial (ADNmt) en células de hepatoblastoma humano (HepG2), células de músculo esquelético (SkMCs) o células epiteliales de túbulo proximal renal. El tenofovir eleva la producción de lactato en menos del 20% en células HepG2 o SkMCs. El tenofovir se fosforila eficientemente a difosfato de tenofovir (TFV-DP) tanto en células HepG2 como en hepatocitos humanos primarios. El tenofovir tiene una concentración efectiva del 50% de 1.1 mM contra el VHB en ensayos basados en células, y la potencia mejora más de 50 veces con la adición de progrupos de bis-isoproxil. El tenofovir ha demostrado previamente actividad completa contra el VHB resistente a la lamivudina in vitro y clínicamente. El tenofovir inhibe la proliferación de células HepG2 derivadas del hígado y células musculares esqueléticas normales con valores de CC(50) de 398 μM y 870 μM, respectivamente. El tenofovir muestra efectos sustancialmente más débiles sobre la proliferación y viabilidad de las células epiteliales del túbulo proximal renal que el cidofovir, un análogo nucleotídico relacionado con el potencial de inducir disfunción tubular renal.
Referencias	[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/

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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

Soporte técnico

Instrucciones de manipulación

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

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Tenofovir Disoproxil Fumarate Reverse Transcriptase inhibidor

Estructura química

Peso molecular: 635.51