1. Membrane Transporter/Ion Channel Autophagy
  2. CFTR Autophagy
  3. Lumacaftor

Lumacaftor  (Synonyms: 鲁玛卡托; VX-809; VRT 826809)

目录号: HY-13262 纯度: 99.83%
COA 产品使用指南

Lumacaftor (VX-809; VRT 826809) 是 CFTR 调节剂,可纠正 CFTR 蛋白的折叠和运输。

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Lumacaftor Chemical Structure

Lumacaftor Chemical Structure

CAS No. : 936727-05-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880
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1 mg ¥363
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5 mg ¥800
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10 mg ¥1100
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50 mg ¥1820
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100 mg ¥2370
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Other Forms of Lumacaftor:

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Top Publications Citing Use of Products

    Lumacaftor purchased from MCE. Usage Cited in: J Physiol Sci. 2019 Jan;69(1):103-112.  [Abstract]

    Effect of VX-809 on maturation of Δ(G970-T1122)-CFTR protein. Immunoblots for WT-, ΔF508-, and Δ(G970-T1122)-CFTR proteins expressed in CHO cells in the presence of 0, 3, or 10 μM VX-809 at a 37°C for 24 h or b 27°C for 48 h.

    Lumacaftor purchased from MCE. Usage Cited in: Sci Rep. 2015 Oct 30;5:15946.  [Abstract]

    VX-809 reverses the heat-induced effects in cells including reduction in CFTR, upregulation of COX-2 and increases in PGE2.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.

    IC50 & Target

    EC50: 0.1 μM (CFTR)[1]

    体外研究
    (In Vitro)

    In fischer rat thyroid (FRT) cells, Lumacaftor improves F508del-CFTR maturation by 7.1±0.3 fold (n=3) compared with vehicle-treated cells (EC50, 0.1±0.1 μM; n=3) and enhances F508del-CFTR-mediated chloride transport by approximately fivefold (EC50, 0.5±0.1 μM; n=3). At Lumacaftor concentrations greater than 10 μM, the response is reduced, resulting in a bell-shaped dose-response relationship with an IC50 of approximately 100 μM. Lumacaftor is orally bioavailable in rats and achieved in vivo plasma levels significantly above concentrations required for in vitro efficacy[1]. Lumacaftor produces a concentration-dependent increase in the HRP luminescence signal after incubation with cells at 37°C or 27°C in both cell lines, with a similar EC50 value of approximately 0.3 µM. In F508-HRP CFBE41o- cells at 37°C, Lumacaftor increases the signal maximally to approximately 250 luminescence arbitrary units (a.u.) over the DMSO control baseline of approximately 60 a.u., representing an approximately 4-fold signal increase. Similarly, with the R1070W-HRP CFBE41o- cells, Lumacaftor increases the signal maximally to approximately 220 a.u. over the DMSO control baseline of approximately 85 a.u., representing an approximately 2.5-fold signal increase. Therefore, both cell lines produced robust signals with a good dynamic range for high-throughput screening[2].

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

    体内研究
    (In Vivo)

    Oral dosing of 1 mg/kg Lumacaftor in male Sprague-Dawley rats results in a Cmax of 2.4±1.3 μM with a t1/2 of 7.7±0.4 h (mean±SD; n=3), indicating that that Lumacaftor is orally bioavailable and able to reach plasma levels that significantly exceeded EC50s for F508del-CFTR correction[1].

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

    Clinical Trial
    分子量

    452.41

    Formula

    C24H18F2N2O5

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    鲁玛卡托

    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 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 25 mg/mL (55.26 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2104 mL 11.0519 mL 22.1038 mL
    5 mM 0.4421 mL 2.2104 mL 4.4208 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, 1 year; -20°C, 6 months。-80°C储存时,请在1个月内使用, -20°C储存时,请在6个月内使用。

    • 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: ≥ 3 mg/mL (6.63 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 30.0 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% Corn Oil

      Solubility: ≥ 3 mg/mL (6.63 mM); 澄清溶液

      此方案可获得 ≥ 3 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.83%

    参考文献
    Kinase Assay
    [2]

    Screening is carried out using a Beckman Coulter Biomek FX platform. In one set of assays, R1070W-F508-CFTR-HRP (R1070W-HRP)-expressing CFBE41o- cells are incubated with 100 µL medium containing 25 µM test compounds and 0.5 μg/mL Doxycycline for 24 hours at 37°C. In a second set of assays, F508-CFTR-HRP (F508-HRP)-expressing CFBE41o- cells are incubated with 100 µL medium containing 25 µM test compounds, 2 µM Lumacaftor, and 0.5 μg/mL doxycycline for 24 hours at 37°C. All compound plates contain negative controls (DMSO) and positive controls (2 µM Lumacaftor). In both assays, the cells are washed four times with PBS, and HRP activity is assayed by the addition of 50 µL/well of HRP substrate. After shaking for 5 minutes, chemiluminescence is measured using a Tecan Infinite M1000 plate reader equipped with an automated stacker (integration time, 100 milliseconds)[2].

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

    Cell Assay
    [2]

    .A549 cells expressing F508-CFTR YFP are grown at 37°C/5% CO2 for 18-24 hours after plating. The cells are then incubated with 100 μL of medium containing test compounds for 18-24 hours. At the time of the assay, cells are washed with PBS and then incubated for 10 minutes with PBS containing forskolin (20 μM) and genistein (50 μM). Each well is assayed individually for I- influx by recording fluorescence continuously (200 milliseconds per point) for 2 seconds (baseline) and then for 12 seconds after rapid addition of 165 μL PBS in which 137 mM Cl- is replaced by I-. The initial I- influx rate is computed by fitting the final 11.5 seconds of the data to an exponential for extrapolation of initial slope, which is normalized for background-subtracted initial fluorescence. All compound plates contain negative controls (DMSO vehicle) and positive controls (5 µM Lumacaftor). Fluorescence is measured using a Tecan Infinite M1000 plate reader equipped with a dual syringe pump (excitation/emission 500/535 nm)[2].

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

    Animal Administration
    [1]

    Rats[1]
    Male rats (n=3 per dose group) are orally administered Lumacaftor in a vehicle consisting of 0.5% Tween80/0.5% methylcellulose/water at a dose volume of 5 mL/kg. The concentration of Lumacaftor in plasma samples is determined with a liquid chromatography/tandem MS method. Pharmacokinetic parameters are calculated byusing WinNonlin Professional Edition software.

    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, 1 year; -20°C, 6 months。-80°C储存时,请在1个月内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2104 mL 11.0519 mL 22.1038 mL 55.2596 mL
    5 mM 0.4421 mL 2.2104 mL 4.4208 mL 11.0519 mL
    10 mM 0.2210 mL 1.1052 mL 2.2104 mL 5.5260 mL
    15 mM 0.1474 mL 0.7368 mL 1.4736 mL 3.6840 mL
    20 mM 0.1105 mL 0.5526 mL 1.1052 mL 2.7630 mL
    25 mM 0.0884 mL 0.4421 mL 0.8842 mL 2.2104 mL
    30 mM 0.0737 mL 0.3684 mL 0.7368 mL 1.8420 mL
    40 mM 0.0553 mL 0.2763 mL 0.5526 mL 1.3815 mL
    50 mM 0.0442 mL 0.2210 mL 0.4421 mL 1.1052 mL
    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:
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    目录号:
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