Home Microbiology Reverse Transcriptase inhibitor - HIV inhibitor - HBV inhibitor Emtricitabine (BW 1592)

Emtricitabine (BW 1592)

Catalog No.S1704 Synonyms: FTC

For research use only.

Emtricitabine (BW1592, 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 (BW 1592) Chemical Structure

CAS No. 143491-57-0

Selleck's Emtricitabine (BW 1592) has been cited by 9 Publications

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Biological Activity

Description Emtricitabine (BW1592, 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepAD38 cell Mn7qSpVv[3Srb36gZZN{[Xl? MlPrTY5pcWKrdHnvckBw\iCqZYDheIl1cXNiQjD2bZJ2eyC{ZYDsbYNifGmxbjDpckB1cGViSHXwRWQ{QCClZXzsJIxqdmVuIFXEOVA:OC5yMzFOwG0> MXKxNVEzQDZ3Mh?=
MT2 cells M3\xemZ2dmO2aX;uJIF{e2G7 M1myN2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiaX7m[YN1\WRiaX6gbJVu[W5iTWSyJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZidnnyZYwhemWybHnjZZRqd25uIFnDOVA:OC5yNESg{txO M2TmR|E6PTl4OEi1
HeLa P4/R5 cells NXHEb5hvTnWwY4Tpc44h[XO|YYm= M2TCRWFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhKXjFiaX7m[YN1\WRiaX6gbJVu[W5iSHXMZUBRPC:UNTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vNCCLQ{WwQVAvOTdizszN Mkm3NVk2QTZ6OEW=
HepG2 cells NGOzTY9EgXSxdH;4bYNqfHliYYPzZZk> MYC5JIRigXN? M3LYbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFkh\GG7czDifUBOXFRiYYPzZZktKEmFNUC9NlcvPyEQvF2= MV6xO|g5QDZ4Mh?=
MDCK2 cells M4HofGZ2dmO2aX;uJIF{e2G7 NGrCbYQyOCEQvF2= NEDrO4ZKdmirYnn0bY9vKG:oIHj1cYFvKE2UUEOg[ZhxemW|c3XkJIlvKE2GQ1uyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGmwdILhZ4VtdHWuYYKgR21HKG[udX;y[ZNk\W6lZTDheEAyOCC3TTDifUBEVU[GQTDhd5NigQ>? MUGxO|E4OjNzMR?=
Click to View More Cell Line Experimental Data

Protocol (from reference)

Solubility (25°C)

In vitro

 DMSO 49 mg/mL
(198.17 mM)
Water 49 mg/mL
(198.17 mM)
Ethanol ''''9 mg/mL

* 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 247.25
Formula

C8H10FN3O3S
CAS No. 143491-57-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C(OC(S1)CO)N2C=C(C(=NC2=O)N)F

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05097430 Recruiting Behavioral: Alcohol-focused brief intervention Hazardous Alcohol Use Centre for Addiction and Mental Health|University Health Network Toronto|Maple Leaf Medical Clinic September 28 2021 Not Applicable
NCT04979728 Recruiting Other: Fingerstick collection of dried blood spots Hiv University of Colorado Denver May 27 2021 --
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)

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