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

Emtricitabine  (Synonyms: 恩曲他濱; BW1592)

目錄號: HY-17427 純度: 99.94%
COA 產(chǎn)品使用指南

Emtricitabine是核苷逆轉(zhuǎn)錄酶抑制劑 (NRTI)， 在PBMC細(xì)胞中的EC50 值為0.01 μM。它可用于 HIV 感染的研究。

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Emtricitabine Chemical Structure

Emtricitabine Chemical Structure

CAS No. : 143491-57-0

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規(guī)格 價格 是否有貨 數(shù)量
25 mg ￥373
In-stock
50 mg ￥500
In-stock
100 mg ￥800
In-stock
500 mg ￥1350
In-stock
1 g   詢價  
5 g   詢價  

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Customer Review

Other Forms of Emtricitabine:

    Emtricitabine purchased from MCE. Usage Cited in: J Neuroimmune Pharmacol. 2017 Dec;12(4):682-692.  [Abstract]

    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.

    Emtricitabine purchased from MCE. 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.

    查看 HIV 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    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

     

    細(xì)胞效力
    (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 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]
    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]
    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 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 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 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 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]
    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]
    體外研究
    (In Vitro)

    Emtricitabine 對 HIV-1 和 HIV-2 的實驗室菌株以及 HIV-1 的臨床分離株均具有體外活性。50% 有效濃度 (EC50) 范圍為 0.002 至 1.5 μmol/L，具體取決于所使用的病毒分離物和細(xì)胞系。Emtricitabine 與齊多夫定和司他夫定體外協(xié)同作用，當(dāng)與扎西他濱或去羥肌苷聯(lián)合使用時體外活性[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    生殖和發(fā)育毒理學(xué)研究是用 Emtricitabine 進行的?？诜┝扛哌_每天一次 1000 mg/kg/day 時，暴露于妊娠動物的每日曲線下面積 (AUC0→24) 約為 60-(小鼠) 至 120 倍 (兔) ，高于人類的推薦劑量 （200 毫克）。在一項小鼠生育力研究中，Emtricitabine 對生育力、精子數(shù)量或早期胚胎發(fā)育沒有影響。在小鼠和兔胚胎胎兒毒理學(xué)研究中沒有增加畸形發(fā)生率。在小鼠產(chǎn)前和產(chǎn)后研究中，F(xiàn)1 后代的發(fā)育和生育能力不受 Emtricitabine 的影響。這些數(shù)據(jù)表明 Emtricitabine 具有良好的臨床前生殖安全性[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    247.25

    Formula

    C8H10FN3O3S
    CAS 號
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    恩曲他濱
    結(jié)構(gòu)分類
    初始來源
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (404.45 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    H2O 中的溶解度 : ≥ 25 mg/mL (101.11 mM)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (10.11 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.11 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    計算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請具體參考實測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.94%

    參考文獻
    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.
    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 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

    * 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

    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.

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    產(chǎn)品名稱：
    Emtricitabine
    目錄號：
    HY-17427
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