Name: Emtricitabine (FTC)
Brand: Selleck Chemicals
SKU: S1704
Rating: 5 (15 reviews)

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

CAS: 143491-57-0

Selleck's Emtricitabine (FTC) has been cited by 15 publications

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Emtricitabine (FTC) Related Products

Related Targets	HBV RT HIV RT RT	Click to Expand
Related Compound Libraries	Anti-infection Compound Library Antibiotics compound Library Antiviral Compound Library Anti-parasitic Compound Library Gut Microbial Metabolite Library	Click to Expand

Signaling Pathway

Reverse Transcriptase Signaling Pathway

Choose Selective Reverse Transcriptase Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06005610	Not yet recruiting	HIV I Infection	National Institute of Allergy and Infectious Diseases (NIAID)	January 2 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
NCT06078228	Enrolling by invitation	Anesthesia	Ain Shams University	September 24 2023	--
NCT05755204	Recruiting	HIV Prevention	Orlando Immunology Center	June 21 2023	--
NCT05957913	Enrolling by invitation	Multiple Sclerosis	Massachusetts General Hospital\|Solving MS	June 5 2023	Phase 2

References

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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% DMSO + % + % Tween 80 + % ddH₂O

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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.
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
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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.

Handling Instructions

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