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Emtricitabine (FTC) NRT inhibitor

Name: Emtricitabine (FTC)
Brand: Selleck Chemicals
SKU: S1704
Availability: InStock
Rating: 5 (21 reviews)

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.

Chemical Structure

Molecular Weight: 247.25

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase Integrase HBV CMV Neuraminidase HCV HSV RSV Enterovirus Thioredoxin Reductase 3C-Like Protease Ribosomal Peptidyl Transferase HPV
Related Products	Dapivirine (TMC120) Salicylanilide Fangchinoline

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	247.25	Formula	C₈H₁₀FN₃O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	143491-57-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BW 1592			Smiles	C1C(OC(S1)CO)N2C=C(C(=NC2=O)N)F

Solubility

In vitro
Batch:

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

Water : 49 mg/mL

Ethanol : 13 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Reverse transcriptase ^[1]
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.^[1] 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.^[2] 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.^[3] Additionally, it exhibits anti-HBV activity in vitro (EC50, 0.01–0.04 µM) that is comparable to the anti-HBV activity of 3TC.^[4] 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.^[5]
References	https://pubmed.ncbi.nlm.nih.gov/18018766/ https://pubmed.ncbi.nlm.nih.gov/16759055/ https://pubmed.ncbi.nlm.nih.gov/11491420/ https://pubmed.ncbi.nlm.nih.gov/16323102/ 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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