Home Microbiology Reverse Transcriptase inhibitor Emtricitabine (FTC)

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Emtricitabine (FTC) NRT inhibitor

Cat.No.S1704

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, and its intracellular half-life is 39 h.
Emtricitabine (FTC) Reverse Transcriptase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 247.25

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Quality Control

Batch: Purity: 99.96%
99.96

Cell Culture, Treatment & Working Concentration

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
MT2 cells Function assay Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.044 μM
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
HepG2 cells Cytotoxicity assay 9 days Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=27.7 μM
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
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Solubility

In vitro
Batch:

DMSO : 49 mg/mL (198.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 49 mg/mL

Ethanol : 13 mg/mL

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.
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Chemical Information, Storage & Stability

Molecular Weight 247.25 Formula

C8H10FN3O3S

 Storage (From the date of receipt)
CAS No. 143491-57-0 Download SDF Storage of Stock Solutions

Synonyms BW 1592 Smiles C1C(OC(S1)CO)N2C=C(C(=NC2=O)N)F

Mechanism of Action

Targets/IC50/Ki
Reverse transcriptase
In vitro
Emtricitabine (FTC) moderately reduces hepatocyte proliferation independent of effects on mtDNA in HepG2 human hepatoma cells, and when combined with tenofovir, slightly reduces cell proliferation without affecting mitochondrial parameters. It efficiently converts to its active metabolites in PBMCs and CEM cells, and displays additive to synergistic activity against HIV replication in PBMCs when combined with tenofovir, resulting in strongly synergistic anti-HIV activity in MT-2 cells against both wild-type and mutant virus. This compound demonstrates antiviral activity against laboratory adapted strains of HIV-1 and HIV-2 in various cell systems, and also exhibits antiviral activity in cell culture against feline and simian immuno-deficiency viruses (SIVs). It consistently shows up to 10-fold greater activity than lamivudine against all viruses tested in all T-cell lines, and generally demonstrates greater potency in vitro in human PBMCs than in MT-4 lines. Additionally, it exhibits anti-HBV activity in vitro (EC50, 0.01–0.04 µM) that is comparable to the anti-HBV activity of 3TC. It 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 this compound. Emtricitabine, lamivudine, and zidovudine are equally active against a panel of eight primary HIV-1 isolates from antiretroviral-naive subjects in PBMCs.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16323102/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12626884/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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