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Tenofovir Alafenamide

Synonyms: GS-1278

Catalog No.S7856 Purity: 99.83%

Tenofovir Alafenamide is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and Hepatitis B.

Tenofovir Alafenamide Chemical Structure

CAS: 379270-37-8

Selleck's Tenofovir Alafenamide has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.83%

99.83

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
MT2 cells	Cytotoxicity assay				Cytotoxicity against human MT2 cells, CC50=40 μM	24686012
Click to View More Cell Line Experimental Data

Biological Activity

Description

Tenofovir Alafenamide is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and Hepatitis B.

Targets

Reverse transcriptase ^[1]

In vitro
In vitro	GS-7340 has a potent anti-HIV activity with IC50 of 0.005 μM. ^[1] GS 7340 has a half-life of 90 min in human plasma and a half-life of 28.3 min in an MT-2 cell extract at 37°C. ^[2] the hepatic uptake of GS-7340 isfacilitated by OATP1B1 and OATP1B3, respectively. GS-7340 inhibits HBV reverse transcriptase after being converted to the pharmacologically active form, TFV-DP. ^[3]

In Vivo
In vivo	In male beagle dogs, GS 7340 (10 mg/kg, p.o.) results in an enhanced distribution to lymphatic tissue. ^[2]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05222945	Not yet recruiting	HIV-1-infection	ANRS Emerging Infectious Diseases\|Gilead Sciences	February 1 2022	Not Applicable
NCT04551573	Withdrawn	Tuberculosis\|Hiv	Yale University\|Gilead Sciences	May 2021	Phase 4

References
[1] Chapman H, et al. Nucleosides Nucleotides Nucleic Acids. 2001, 20(4-7), 1085-10[90. [2] Lee WA, et al. Antimicrob Agents Chemother. 2005, 49(5), 1898-1906. [3] Murakami E, et al. Antimicrob Agents Chemother. 2015, 59(6), 3563-3569.

References

Chemical lnformation & Solubility

Molecular Weight	476.47	Formula	C₂₁H₂₉N₆O₅P
CAS No.	379270-37-8	SDF	Download Tenofovir Alafenamide SDF
Smiles	CC(C)OC(=O)C(C)NP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OC3=CC=CC=C3
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 : 95 mg/mL ( (199.38 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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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

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