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Tenofovir

Name: Tenofovir
Brand: Selleck Chemicals
SKU: S1401
Rating: 5 (28 reviews)

Synonyms: GS-1278

Catalog No.S1401 Purity:99.98%

Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.

Tenofovir Chemical Structure

CAS No. 147127-20-6

Purity & Quality Control

Batch: Purity: 99.98%

99.98

Tenofovir Related Products

Related Targets	HBV RT HIV RT RT	Click to Expand
Related Products	Dapivirine (TMC120) Salicylanilide Fangchinoline	Click to Expand
Related Compound Libraries	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	Click to Expand

Signaling Pathway

Reverse Transcriptase Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
human MT2 cells	Function assay		5 days	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay, EC50=0.013 μM	20409721
human H9 cells	Function assay			Antiviral activity against HIV1 clade F isolate 2338 infected in human H9 cells assessed as inhibition of viral replication, EC50=0.04 μM	21803462
C3H/3T3 cells	Function assay		6 days	Inhibition of murine sarcoma virus-induced transformation of mouse embryo fibroblast C3H/3T3 cells after 6 days, EC50=0.23 μM	18556209
CEM (human leukemia) cells	Function assay			Antiviral activity against HIV-1 (IIIB) in CEM (human leukemia) cells, EC50=1.2 μM	14584956
MT-4 cells	Function assay			In vitro antiviral activity against HIV-2 in MT-4 cells, EC50=1.4 μM	11327587
human bone marrow cells	Cytotoxicity assay		24 h	Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=3.5 μM	20439609
C8166 cells	Function assay		4 days	Antiviral activity against 100 TCID50 wild-type Human immunodeficiency virus type 2 ROD infected in C8166 cells assessed as inhibition of syncytia formation after 4 days by microscopic analysis, EC50=7.1 μM	21803462
mouse L1210 cells	Cytotoxicity assay		48 h	Cytostatic activity against mouse L1210 cells after 48 hrs by coulter counting analysis, IC50=11 μM	24686012
human HepG2 cells	Function assay		9 days	Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=12.3 μM	17888662
human HeLa cells	Cytotoxicity assay		72 h	Cytostatic activity against human HeLa cells after 72 hrs by coulter counting analysis, IC50=17 μM	24686012
CHO cells	Cytotoxicity assay		120 h	Cytotoxicity against CHO cells after 120 hrs by Cell-Titer Glo assay, CC50=21 μM	19001108
MDCK2 cells	Function assay	10 μM		Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay	17172311
human HepG2 cells	Cytotoxicity assay		14 days	Cytotoxicity against human HepG2 cells assessed as inhibition of cellular DNA replication after 14 days	20409721
Click to View More Cell Line Experimental Data

Biological Activity

Description

Tenofovir (GS-1278) blocks reverse transcriptase and hepatitis B virus infections.

Features

Tenofovir disoproxil fumarate is the prodrug form of tenofovir.

Targets

Reverse transcriptase ^[1]

In vitro
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. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). ^[1] Tenofovir is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. ^[2] Tenofovir inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. ^[3] Tenofovir (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir 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. ^[4]

In Vivo
In vivo	Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir treatment 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. Tenofovir (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques. ^[5]
Animal Research	Animal Models	Macaques
	Dosages	30 mg/kg
	Administration	Subcutaneously

References

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Chemical Information & Solubility

Molecular Weight	287.21	Formula	C₉H₁₄N₅O₄P
CAS No.	147127-20-6	SDF	Download Tenofovir SDF
Smiles	CC(CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 4 mg/mL ( (13.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 2 mg/mL

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Clear solution	saline	2.000mg/ml (6.96mM)	Taking the 1 mL working solution as an example, add 2 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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.
Clear solution	saline	2.000mg/ml (6.96mM)	Taking the 1 mL working solution as an example, add 2 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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.
Clear solution	saline	33.000mg/ml (114.90mM)	Taking the 1 mL working solution as an example, add 33 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	30%propylene glycol 1 5%Tween80 2 65%D5W Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (104.45mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	saline	4.000mg/ml (13.93mM)	Taking the 1 mL working solution as an example, add 4 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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