1. Anti-infection
  2. HIV
    Reverse Transcriptase

Emtricitabine (Synonyms: BW1592)

Cat. No.: HY-17427 Purity: 99.60%
Data Sheet SDS Handling Instructions

Emtricitabine is an inhibitor of the nucleoside reverse transcriptase (NRTI) and human immunodeficiency virus type 1 (HIV-1); inhibits NRTI with an EC50 of 0.01 µM in PBMC cell.

For research use only. We do not sell to patients.
Emtricitabine Chemical Structure

Emtricitabine Chemical Structure

CAS No. : 143491-57-0

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10 mM * 1 mL in DMSO $61 In-stock
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200 mg $130 In-stock
500 mg $260 In-stock
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    Emtricitabine purchased from MCE. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.

    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.

    Emtricitabine purchased from MCE. Usage Cited in: J Neuroimmune Pharmacol. 2017 Jul 22.

    TDF/FTC/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.
    • Biological Activity

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    Description

    Emtricitabine is an inhibitor of the nucleoside reverse transcriptase (NRTI) and human immunodeficiency virus type 1 (HIV-1); inhibits NRTI with an EC50 of 0.01 µM in PBMC cell.

    IC50 & Target

    EC50: 0.01 µM (NRTI, PBMC), 0.026 µM (NRTI, HeLa cell)[1]

    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].

    In Vivo

    Reproductive and developmental toxicology studies are conducted with emtricitabine. Oral doses up to 1000 mg/kg/day provided daily area under the curve (AUC0→24) exposure to pregnant animals approximately 60- (mice) to 120-fold (rabbits) higher than that in humans at the recommended dose of 200 mg given once per day. In a mouse fertility study, emtricitabine had no effect on fertility, sperm count, or early embryonic development. There is no increased incidence of malformations in mouse and rabbit embryofetal toxicology studies. The development and fertility of F1 progeny are unaffected by emtricitabine in a mouse pre- and post-natal study. These data demonstrate a favorable pre-clinical reproductive safety profile for emtricitabine[2].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 4.0445 mL 20.2224 mL 40.4449 mL
    5 mM 0.8089 mL 4.0445 mL 8.0890 mL
    10 mM 0.4044 mL 2.0222 mL 4.0445 mL
    Please refer to the solubility information to select the appropriate solvent.
    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]. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

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    Product Name:
    Emtricitabine
    Cat. No.:
    HY-17427
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