2. Anti-infection Metabolic Enzyme/Protease
  3. HIV Reverse Transcriptase Endogenous Metabolite
  4. Emtricitabine

Emtricitabine  (Synonyms: BW1592)

製品番号: HY-17427 純度: 99.97%
COA 取扱説明書 Technical Support

Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.

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CAS 番号 : 143491-57-0

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10 mM * 1 mL in DMSO
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100 mg $88 在庫あり
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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Emtricitabine:

Emtricitabine 関連抗体

Top Publications Citing Use of Products

    Emtricitabine purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Aug 26:101702.  [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.

    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.

    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.

    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.

    HIV アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    HIV HIV-1 HIV-2

    Endogenous Metabolite アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    Human Endogenous Metabolite Microbial Metabolite

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with an EC50 of 0.01 μM in PBMC cell. It is an antiviral agent for the treatment of HIV infection.

    IC50 & Target

    HIV-1

     

    HIV-2

     

    Cellular Effect
    Cell Line Type Value Description References
    CCRF-CEM CC50
    >100 μM
    Compound: 1d; FTC
    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
    		[PMID: 32515595]
    CCRF-CEM CC50
    >100 μM
    Compound: 3; (-)-FTC
    Cytotoxicity against human CEM cells measured after 6 days
    Cytotoxicity against human CEM cells measured after 6 days
    		[PMID: 37393791]
    CCRF-CEM EC50
    0.04 μM
    Compound: FTC
    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
    		[PMID: 26878150]
    CCRF-CEM ED50
    >50 μM
    Compound: beta-L-SddC (3TC)
    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
    		[PMID: 8627596]
    CCRF-CEM ED50
    50 μM
    Compound: beta-L-SddC (3TC)
    In vitro concentration required to inhibit 50% of CEM cell growth
    In vitro concentration required to inhibit 50% of CEM cell growth
    		[PMID: 8627596]
    HeLa EC50
    >404 μM
    Compound: 36, FTC, Emtricitabine
    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
    		[PMID: 22352809]
    HeLa EC50
    0.8 μM
    Compound: 36, FTC, Emtricitabine
    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
    		[PMID: 22352809]
    HeLa EC50
    2 μM
    Compound: 36, FTC, Emtricitabine
    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
    		[PMID: 22352809]
    HeLa IC50
    0.17 μM
    Compound: FTC
    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
    		[PMID: 19596885]
    HepG2 CC50
    765 μM
    Compound: FTC
    Cytotoxicity against human HepG2 cells after 3 days by MTT assay
    Cytotoxicity against human HepG2 cells after 3 days by MTT assay
    		[PMID: 17404006]
    HepG2 EC50
    0.03 μM
    Compound: FTC
    Inhibition of hepatitis B virus replication in the HepAD38 cell line.
    Inhibition of hepatitis B virus replication in the HepAD38 cell line.
    		[PMID: 11128652]
    HepG2 ED50
    17 nM
    Compound: beta-L-SddC (3TC)
    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
    		[PMID: 8627596]
    HepG2 ED50
    30 nM
    Compound: beta-L-SddC (3TC)
    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
    		[PMID: 8627596]
    HepG2 IC50
    27.7 μM
    Compound: emtricitabine
    Cytotoxicity against human HepG2 cells after 9 days by MTT assay
    Cytotoxicity against human HepG2 cells after 9 days by MTT assay
    		[PMID: 17888662]
    HepG2 2.2.15 EC50
    0.1 μM
    Compound: FTC
    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
    		[PMID: 17404006]
    HL-60 CC50
    845 μM
    Compound: FTC
    Cytotoxicity against human HL60 cells after 3 days by MTT assay
    Cytotoxicity against human HL60 cells after 3 days by MTT assay
    		[PMID: 17404006]
    MT2 EC50
    323 nM
    Compound: FTC
    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
    		[PMID: 19104010]
    MT2 ED50
    2 μM
    Compound: beta-L-SddC (3TC)
    Concentration required to inhibit 50% of HIV activity in MT-2 cells
    Concentration required to inhibit 50% of HIV activity in MT-2 cells
    		[PMID: 8627596]
    MT2 IC50
    0.044 μM
    Compound: FTC
    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
    		[PMID: 19596885]
    PBMC CC50
    >10 μM
    Compound: FTC
    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
    		[PMID: 34795872]
    PBMC CC50
    >200 μM
    Compound: 3; (-)-FTC
    Cytotoxicity against PBMC (unknown origin)
    Cytotoxicity against PBMC (unknown origin)
    		[PMID: 37393791]
    Vero IC50
    >100 μM
    Compound: 51
    Cytotoxicity was determined in the vero cells infected with HIV-I
    Cytotoxicity was determined in the vero cells infected with HIV-I
    		[PMID: 8423591]
    体外実験

    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.

    Emtricitabine 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    247.25

    分子式

    C8H10FN3O3S
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1N=C(N)C(F)=CN1[C@@H]2CS[C@H](CO)O2
    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    純度とドキュメンテーション

    純度: 99.97%

    COA (251 KB) HNMR (257 KB) RP-HPLC (230 KB) LCMS (330 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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.

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    Emtricitabine Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Emtricitabine143491-57-0BW1592BW 1592BW-1592HIVReverse TranscriptaseEndogenous MetaboliteHuman immunodeficiency virusInhibitorinhibitorinhibit

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    製品番号:
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