Tenofovir Alafenamide (GS-7340)

Catalog No.S7856

For research use only.

Tenofovir Alafenamide (GS-7340) is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and Hepatitis B.

Tenofovir Alafenamide (GS-7340) Chemical Structure

CAS No. 379270-37-8

Selleck's Tenofovir Alafenamide (GS-7340) has been cited by 7 Publications

Purity & Quality Control

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Biological Activity

Description Tenofovir Alafenamide (GS-7340) is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and Hepatitis B.
Targets
Reverse transcriptase [1]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MT2 cells M3niVWN6fG:2b4jpZ4l1gSCjc4PhfS=> NGfVSYZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOXDJiY3XscJMtKEOFNUC9OFAh|ryP NIXidWwzPDZ6NkCxNi=>
In vivo In male beagle dogs, GS 7340 (10 mg/kg, p.o.) results in an enhanced distribution to lymphatic tissue. [2]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 95 mg/mL
(199.38 mM)
Ethanol 95 mg/mL
(199.38 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 476.47
Formula

C21H29N6O5P

CAS No. 379270-37-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)OC(=O)C(C)NP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OC3=CC=CC=C3

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04551573 Withdrawn Drug: Rifapentine daily|Drug: Rifapentine weekly Tuberculosis|Hiv Yale University|Gilead Sciences May 2021 Phase 4
NCT04530630 Recruiting Drug: BIKTARVY 50Mg-200Mg-25Mg Tablet HIV Infections|Renal Transplant Rejection Weill Medical College of Cornell University|Gilead Sciences November 9 2020 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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