Tenofovir Alafenamide (GS-7340)

Catalog No.S7856

Tenofovir Alafenamide (GS-7340) Chemical Structure

Molecular Weight(MW): 476.47

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

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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 M3LT[2N6fG:2b4jpZ4l1gSCjc4PhfS=> MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWFIh[2WubIOsJGNEPTB;NECg{txO NG\HXVQzPDZ6NkCxNi=>

... Click to View More Cell Line Experimental Data

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

Protocol

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 powder
Synonyms N/A

Bio Calculators

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03048422 Not yet recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) April 30, 2017 Phase 3
NCT02957994 Not yet recruiting Hepatitis B Asian Pacific Liver Center at St. Vincent Medical Center February 2017 Phase 4
NCT02984852 Recruiting Healthy Janssen Scientific Affairs, LLC December 2016 Phase 1
NCT02962739 Not yet recruiting Healthy Volunteers University of Colorado, Denver December 2016 Phase 1
NCT02957864 Recruiting Renal Insufficiency,Chronic|Hiv|Therapeutic Agent Toxicity Erasmus Medical Center|Gilead Sciences October 2016 Phase 4
NCT02904369 Recruiting HIV CONRAD|United States Agency for International Development (USAID)|Agility Clinical, Inc. October 2016 Phase 1

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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Reverse Transcriptase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID