Home Microbiology Reverse Transcriptase inhibitor - HIV inhibitor - HBV inhibitor Emtricitabine (FTC) For research use only.

Emtricitabine (FTC)

Synonyms: BW 1592

Emtricitabine (FTC) is a new nucleoside agent that has activity against both human immunodeficiency virus (HIV) and hepatitis B virus. It is a reverse transcriptase inhibitor. Intracellular half-life is 39 h.

Emtricitabine (FTC) Chemical Structure

Emtricitabine (FTC) Chemical Structure

CAS No. 143491-57-0

Purity & Quality Control

Emtricitabine (FTC) Related Products

Signaling Pathway

Reverse Transcriptase Signaling Pathways

Reverse Transcriptase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepAD38 cell Function assay Inhibition of hepatitis B virus replication in the HepAD38 cell line, ED50=0.03 μM 11128652
MT2 cells Function assay Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.044 μM 19596885
HeLa P4/R5 cells Function assay Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=0.17 μM 19596885
HepG2 cells Cytotoxicity assay 9 days Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=27.7 μM 17888662
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
Click to View More Cell Line Experimental Data

Biological Activity

Description Emtricitabine (FTC) is a new nucleoside agent that has activity against both human immunodeficiency virus (HIV) and hepatitis B virus. It is a reverse transcriptase inhibitor. Intracellular half-life is 39 h.
Targets
Reverse transcriptase [1]
In vitro
In vitro Emtricitabine moderately reduces hepatocyte proliferation independent of effects on mtDNA in HepG2 human hepatoma cells. Emtricitabine plus tenofovir slightly reduced cell proliferation without affecting mitochondrial parameters. [1] Emtricitabine efficiently converts to their active metabolites in PBMCs and CEM cells. Emtricitabine combined with Tenofovir displays additive to synergistic activity against HIV replication in PBMCs and results in strongly synergistic anti-HIV activity in MT-2 cells against both wild-type and mutant virus. [2] Emtricitabine demonstrates antiviral activity against laboratory adapted strains of HIV-1 and HIV-2 in various cell system. Emtricitabine also exhibits antiviral activity in cell culture against feline and simian immuno-deficiency viruses (SIVs). Emtricitabine consistently exhibits up to 10-fold greater activity than lamivudine against all viruses tested in all T-cell lines. Emtricitabine generally demonstrates greater potency in vitro in human PBMCs than in MT-4 lines. [3] Emtricitabine also exhibits anti-HBV activity in vitro (EC50, 0.01–0.04 µM) that is comparable to the anti-HBV activity of 3TC. [4] Emtricitabine is approximately fourfold more active than 3TC in assays in the transformed T-cell line MT-4 infected with HIV-(1IIIB), whereas Zidovudine is more active than Emtricitabine. Emtricitabine, Lamivudine and Zidovudine are equally active against a panel of eight primary HIV-1 isolates from antiretroviral-naive subjects in PBMCs. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06005610 Recruiting
HIV I Infection
National Institute of Allergy and Infectious Diseases (NIAID)
 January 4 2024 Phase 2
NCT05924438 Recruiting
HIV-1-infection
Professor Francois Venter|Africa Health Research Institute|Merck Sharp & Dohme LLC|University of Witwatersrand South Africa
 November 8 2023 Phase 3

Chemical Information & Solubility

Molecular Weight 247.25 Formula

C8H10FN3O3S
CAS No. 143491-57-0 SDF Download Emtricitabine (FTC) SDF
Smiles C1C(OC(S1)CO)N2C=C(C(=NC2=O)N)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 49 mg/mL ( (198.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 49 mg/mL

Ethanol : 49 mg/mL


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In vivo
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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.

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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.

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