Emtricitabine
Based on 8 publication(s) in Google Scholar
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 value of 0.01 μM in PBMC cells. Emtricitabine inhibits HIV reverse transcriptase, preventing RNA from being transcribed into DNA. Emtricitabine has low brain permeability (logP <0)[1][2][3][4][5].
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 143491-57-0
- Formula: C8H10FN3O3S
- Molecular Weight:247.25
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Emtricitabine
More- Cell Rep Med. 2024 Sep 17;5(9):101702. [Abstract]
- J Neuroimmune Pharmacol. 2021 Mar;16(1):159-168. [Abstract]
- J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- ACS Infect Dis. 2025 Oct 30. [Abstract]
- SSRN. 2026 Jun 23.
- bioRxiv. 2025 Aug 14:2025.08.14.670267. [Abstract]
- Open Virol J. 2014 Mar 7:8:1-8. [Abstract]
Customer Validation & Images
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Microbiological Assay
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ELISA
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WB
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WB
Biological Activity
Description
IC50 & Target
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HIV-1 |
HIV-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | CC50 |
>100 μM
Compound: 1d; FTC
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Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability incubated for 4 to 5 days
Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability incubated for 4 to 5 days
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[PMID: 32515595] |
| CCRF-CEM | CC50 |
>100 μM
Compound: 3; (-)-FTC
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Cytotoxicity against human CEM cells measured after 6 days
Cytotoxicity against human CEM cells measured after 6 days
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[PMID: 37393791] |
| CCRF-CEM | EC50 |
0.04 μM
Compound: FTC
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Antiviral activity against subtype B X4 tropic HIV1 3B infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
Antiviral activity against subtype B X4 tropic HIV1 3B infected in GFP-positive human CEM cells expressing CD4+,CXCR4 and CCR5 after 3 days
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[PMID: 26878150] |
| CCRF-CEM | ED50 |
>50 μM
Compound: beta-L-SddC (3TC)
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In vitro concentration required to decrease 50% of mitochondrial DNA content in CEM cells
In vitro concentration required to decrease 50% of mitochondrial DNA content in CEM cells
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[PMID: 8627596] |
| CCRF-CEM | ED50 |
50 μM
Compound: beta-L-SddC (3TC)
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In vitro concentration required to inhibit 50% of CEM cell growth
In vitro concentration required to inhibit 50% of CEM cell growth
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[PMID: 8627596] |
| HeLa | EC50 |
>404 μM
Compound: 36, FTC, Emtricitabine
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Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay
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[PMID: 22352809] |
| HeLa | EC50 |
0.8 μM
Compound: 36, FTC, Emtricitabine
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Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
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[PMID: 22352809] |
| HeLa | EC50 |
2 μM
Compound: 36, FTC, Emtricitabine
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Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay
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[PMID: 22352809] |
| HeLa | IC50 |
0.17 μM
Compound: FTC
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Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication
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[PMID: 19596885] |
| HepG2 | CC50 |
765 μM
Compound: FTC
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Cytotoxicity against human HepG2 cells after 3 days by MTT assay
Cytotoxicity against human HepG2 cells after 3 days by MTT assay
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[PMID: 17404006] |
| HepG2 | EC50 |
0.03 μM
Compound: FTC
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Inhibition of hepatitis B virus replication in the HepAD38 cell line.
Inhibition of hepatitis B virus replication in the HepAD38 cell line.
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[PMID: 11128652] |
| HepG2 | ED50 |
17 nM
Compound: beta-L-SddC (3TC)
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Concentration required to inhibit 50% of extracellular circular replication of HBV DNA using 2215 cell line
Concentration required to inhibit 50% of extracellular circular replication of HBV DNA using 2215 cell line
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[PMID: 8627596] |
| HepG2 | ED50 |
30 nM
Compound: beta-L-SddC (3TC)
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Concentration required to inhibit 50% of intracellular circular replication of HBV DNA using 2215 cell line
Concentration required to inhibit 50% of intracellular circular replication of HBV DNA using 2215 cell line
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[PMID: 8627596] |
| HepG2 | IC50 |
27.7 μM
Compound: emtricitabine
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Cytotoxicity against human HepG2 cells after 9 days by MTT assay
Cytotoxicity against human HepG2 cells after 9 days by MTT assay
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[PMID: 17888662] |
| HepG2 2.2.15 | EC50 |
0.1 μM
Compound: FTC
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Antiviral activity against HBV in HepG2.2.15 cells assessed as decrease in extracellular viral DNA level by RT-PCR
Antiviral activity against HBV in HepG2.2.15 cells assessed as decrease in extracellular viral DNA level by RT-PCR
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[PMID: 17404006] |
| HL-60 | CC50 |
845 μM
Compound: FTC
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Cytotoxicity against human HL60 cells after 3 days by MTT assay
Cytotoxicity against human HL60 cells after 3 days by MTT assay
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[PMID: 17404006] |
| MT2 | EC50 |
323 nM
Compound: FTC
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Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS
Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS
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[PMID: 19104010] |
| MT2 | ED50 |
2 μM
Compound: beta-L-SddC (3TC)
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Concentration required to inhibit 50% of HIV activity in MT-2 cells
Concentration required to inhibit 50% of HIV activity in MT-2 cells
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[PMID: 8627596] |
| MT2 | IC50 |
0.044 μM
Compound: FTC
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Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication
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[PMID: 19596885] |
| PBMC | CC50 |
>10 μM
Compound: FTC
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Cytotoxicity against human PBMC cells assessed as cell viability measured after 11 days by Viacount assay
Cytotoxicity against human PBMC cells assessed as cell viability measured after 11 days by Viacount assay
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[PMID: 34795872] |
| PBMC | CC50 |
>200 μM
Compound: 3; (-)-FTC
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Cytotoxicity against PBMC (unknown origin)
Cytotoxicity against PBMC (unknown origin)
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[PMID: 37393791] |
| Vero | IC50 |
>100 μM
Compound: 51
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Cytotoxicity was determined in the vero cells infected with HIV-I
Cytotoxicity was determined in the vero cells infected with HIV-I
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[PMID: 8423591] |
In Vitro
Emtricitabine has in vitro activity against both laboratory strains of HIV-1 and HIV-2 and clinical isolates of HIV-1. The 50% effective concentration (EC50) ranges from 0.002 to 1.5 μ mol/L, depending on the viral isolate and cell line used. Emtricitabine demonstrates in vitro synergy with zidovudine and stavudine and additive in vitro activity when combines with zalcitabine or didanosine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 143491-57-0
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Appearance Solid
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Molecular Weight 247.25
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Formula C8H10FN3O3S
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Color White to off-white
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SMILES
O=C1N=C(N)C(F)=CN1[C@@H]2CS[C@H](CO)O2
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Synonyms
BW1592
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Decoupling HIV-1 antiretroviral drug inhibition from plasma antibody activity to evaluate broadly neutralizing antibody therapeutics and vaccines. [Abstract]2024 Sep 17;5(9):101702. PMID: 39216479
Emtricitabine purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Sep 17;5(9):101702. [Abstract]
Inhibition of MuLV-pseudotyped HIVpv-WT and HIVpv-MDR viruses by different ARVs. Heatmap depicts mean inhibitory concentration 50 (IC50) values from two independent experiments. Compound mix: efavirenz (EFV), Emtricitabine (FTC), dolutegravir (DTG), and darunavir (DRV) were combined and titrated.
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J Neuroimmune Pharmacol
2021 Mar;16(1):159-168. PMID: 31338753
Emtricitabine purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2021 Mar;16(1):159-168. [Abstract]
Levels of Aβ 1-40 from the media of cultured neurons after ART compounds treatment for 48 h were detected by ELISA. Δ secreted Aβ1-40 represented the difference of secreted Aβ1-40 between ARTs and DMSO (vehicle controls). Lamivudine (1 μM), Emtricitabine (0.1 μM), tenofovir disoproxil (10 μM), ritonavir (1 μM), nelfinavir (1 μM), darunavir (0.1 μM), efavirenz (1 μM), nevirapine (1 μM), dolutegravir (1 μM) and elvitegravir (1 μM) significantly increased secreted Aβ1-40, whereas zidovudine (10 μM) and abacavir (10 μM) significantly decreased secreted Aβ1-40.
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J Neuroimmune Pharmacol
Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. [Abstract]2017 Dec;12(4):682-692. PMID: 28735382
Emtricitabine purchased from MedChemExpress. Usage Cited in: J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Abstract]
TDF/FTC (Emtricitabine)/RAL combined medication induces mouse NPC apoptosis in vitro. Mouse NPCs are treated with either DMSO or TDF/FTC/RAL for 8 h. Cleaved Caspase-3 levels are determined by Western blotting.
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Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
ACS Infect Dis
Targeting the Rift Valley Fever Virus Polymerase: Resistance Mechanisms and Structural Insights. [Abstract]2025 Oct 30. PMID: 41166549 -
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bioRxiv
Mechanistic insights and in vivo HIV suppression by the BRD4-targeting small molecule ZL0580. [Abstract]2025 Aug 14:2025.08.14.670267. PMID: 40832229 -
Open Virol J
Both Cyclophilin Inhibitors and Direct-Acting Antivirals Prevent PKR Activation in HCV-Infected Cells. [Abstract]2014 Mar 7:8:1-8. PMID: 24799968
Emtricitabine purchased from MedChemExpress. Usage Cited in: Open Virol J. 2014 Mar 7:8:1-8. [Abstract]
The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (cyclosporine A and alisporivir), DAAs (the HCV NS5A inhibitor daclatasvir and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor Emtricitabine). Results are representative of 4 independent experiments.
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (404.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 25 mg/mL (101.11 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Cell Assay[3]
EA.hy926 cells were plated in a 12-, 24- or 96-well plates and grown in DMEM media supplemented with 3% FCS. Endothelial cells from PARP+/+and PARP-/- mice were isolated and cultured. Cell viability was determined by the reduction of yellow MTT into a purple formazan product by mitochondrial dehydrogenases of metabolically active cells. Following the treatment period, the experimental medium was removed and 100 μL MTT (1 mg/mL) added. After 1 h incubation, the MTT solution was carefully removed and the purple crystals were solubilized in 100 μL of DMSO. The DMSO was transferred to an ELISA plate and absorbance measured at 550 nm with a 620 nm[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[2]
Mice: Emtricitabine (free base) is suspended in 0.5% aqueous methylcellulose and given by gavage, with the daily dose divided into two equal installments administered approximately 6 h apart. The dose volume is 5 mL/kg/dose (10 mL/kg/day). In 1- and 6-month oral toxicity studies in mice, the maximum tolerated dose of emtricitabine is >3000 mg/kg/day. However, dose-range-finding studies are performed in pregnant CD-1 mice and in New Zealand White rabbits at top doses of 1000 mg/kg/day[2]. Rabbits: Mature artificially inseminated rabbits are given emtricitabine on gestational day 7 through 19. On gestational day 19, blood samples for toxicokinetics are taken from five satellite does in each group at 30–60 min prior to dosing, and at 1, 3, 7, and 12 h after the first daily-dose (prior to the second daily-dose). On gestational day 20, the satellite does are sacrificed at 1 h after the final dose, and maternal blood and fetal umbilical blood samples are collected for toxicokinetics[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (293 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Saag MS, et al. Emtricitabine, a new antiretroviral agent with activity against HIV and hepatitis B virus. Clin Infect Dis.?2006 Jan 1;42(1):126-31. [Content Brief]
[2]. Xu P, et al. Combined Medication of Antiretroviral Drugs Tenofovir Disoproxil Fumarate, Emtricitabine, and Raltegravir Reduces Neural Progenitor Cell Proliferation In Vivo and In Vitro. J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692. [Content Brief]
[3]. Szczech GM, Wang LH, Walsh JP, Reproductive toxicology profile of emtricitabine in mice and rabbits. Reprod Toxicol. 2003 Jan-Feb;17(1):95-108. [Content Brief]
[4]. Faltz M, et al. Effect of the Anti-retroviral Drugs Efavirenz, Tenofovir and Emtricitabine on Endothelial Cell Function: Role of PARP. Cardiovasc Toxicol. 2017 Jan 3. [Epub ahead of print] [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.0445 mL | 20.2224 mL | 40.4449 mL | 101.1122 mL |
| 5 mM | 0.8089 mL | 4.0445 mL | 8.0890 mL | 20.2224 mL | |
| 10 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL | 10.1112 mL | |
| 15 mM | 0.2696 mL | 1.3482 mL | 2.6963 mL | 6.7408 mL | |
| 20 mM | 0.2022 mL | 1.0111 mL | 2.0222 mL | 5.0556 mL | |
| 25 mM | 0.1618 mL | 0.8089 mL | 1.6178 mL | 4.0445 mL | |
| 30 mM | 0.1348 mL | 0.6741 mL | 1.3482 mL | 3.3704 mL | |
| 40 mM | 0.1011 mL | 0.5056 mL | 1.0111 mL | 2.5278 mL | |
| 50 mM | 0.0809 mL | 0.4044 mL | 0.8089 mL | 2.0222 mL | |
| 60 mM | 0.0674 mL | 0.3370 mL | 0.6741 mL | 1.6852 mL | |
| 80 mM | 0.0506 mL | 0.2528 mL | 0.5056 mL | 1.2639 mL | |
| 100 mM | 0.0404 mL | 0.2022 mL | 0.4044 mL | 1.0111 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Emtricitabine Related Classifications
HY-17427 Related Classifications
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