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

Emtricitabine  (Synonyms: 恩曲他滨; BW1592)

目录号: HY-17427 纯度: 99.94%
COA 产品使用指南

Emtricitabine是核苷逆转录酶抑制剂 (NRTI), 在PBMC细胞中的EC50 值为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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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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50 mg ¥500
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100 mg ¥800
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500 mg ¥1350
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5 g   询价  

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Top Publications Citing Use of Products

    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.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    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

     

    体外研究
    (In Vitro)

    Emtricitabine 对 HIV-1 和 HIV-2 的实验室菌株以及 HIV-1 的临床分离株均具有体外活性。50% 有效浓度 (EC50) 范围为 0.002 至 1.5 μmol/L,具体取决于所使用的病毒分离物和细胞系。Emtricitabine 与齐多夫定和司他夫定体外协同作用,当与扎西他滨或去羟肌苷联合使用时体外活性[1]

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

    体内研究
    (In Vivo)

    生殖和发育毒理学研究是用 Emtricitabine 进行的。口服剂量高达每天一次 1000 mg/kg/day 时,暴露于妊娠动物的每日曲线下面积 (AUC0→24) 约为 60-(小鼠) 至 120 倍 (兔) ,高于人类的推荐剂量 (200 毫克)。在一项小鼠生育力研究中,Emtricitabine 对生育力、精子数量或早期胚胎发育没有影响。在小鼠和兔胚胎胎儿毒理学研究中没有增加畸形发生率。在小鼠产前和产后研究中,F1 后代的发育和生育能力不受 Emtricitabine 的影响。这些数据表明 Emtricitabine 具有良好的临床前生殖安全性[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 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    恩曲他滨

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (404.45 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.94%

    参考文献
    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.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 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

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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    产品名称:
    Emtricitabine
    目录号:
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