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Lumacaftor

产品编号 T2595 CAS 936727-05-8

别名: 鲁玛卡托, VRT 826809, VX-809

Lumacaftor 是一种 CFTR 调节剂，可纠正 CFTR 蛋白的折叠和运输。它增强了 FRT 细胞中 F508del-CFTR 蛋白的成熟，EC50为100 nM。

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Lumacaftor, CAS 936727-05-8

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生物活性

化学信息

存储 & 溶解度

参考文献

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产品描述	VX-809 is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM).
靶点活性	F508del-CFTR:0.1 μM (EC50, Fischer rat thyroid cells)
体外活性	In cultured human bronchial epithelial cells isolated from patients with CF homozygous for F508del, Lumacaftor (VX-809) improved F508del-CFTR processing in the endoplasmic reticulum and enhanced chloride secretion to approximately 14% of non-CF human bronchial epithelial cells (EC50: 81 nM), a level associated with mild CF in patients with less disruptive CFTR mutations [1]. VX-809 produced 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 [2].
激酶实验	In one set of assays, R1070W-?F508-CFTR-HRP (R1070W-HRP)–expressing CFBE41o? cells were 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 were incubated with 100 μl medium containing 25 μM test compounds, 2 μM VX-809, and 0.5 μg/ml doxycycline for 24 hours at 37°C. All compound plates contained negative controls (DMSO vehicle) and positive controls [2 μM VX-809]. In both assays, the cells were washed four times with PBS, and HRP activity was assayed by the addition of 50 μl/well of HRP substrate. After shaking for 5 minutes, chemiluminescence was measured using a Tecan Infinite M1000 plate reader (Tecan Groups Ltd, Mannedorf, Switzerland) equipped with an automated stacker (integration time, 100 milliseconds). Z′ is defined as = 1 ? [(3 × standard deviation of maximum signal control + 3 × standard deviation of minimum signal control)/absolute (mean of maximum signal control ? mean of minimum signal control)] [2].
细胞实验	FRT, HEK-293, or HBE cells expressing CFTR or F508del-CFTR were incubated for 24 h at 37 °C with or without VX-809 in the assay media. After incubation, cells were harvested in ice-cold D-PBS solution (without calcium and magnesium) and pelleted at 1,000 × g at 4 °C. Cell pellets were lysed in 1% Nonidet P-40, 0.5% sodium deoxycholate, 200 mM NaCl, 10 mM Tris, pH 7.8, and 1 mM EDTA plus protease inhibitor mixture (1:250) for 30 min on ice. Lysates were spun for 10 min at 10,000 × g at 4 °C to pellet nuclei and insoluble material. Approximately 12 μg total protein was heated in Laemmli buffer with 5% β-mercaptoethanol at 37 °C for 5 min and loaded onto a 3% to 8% Tris-acetate gel. The gel was transferred to nitrocellulose and processed for Western blotting by using monoclonal CFTR antibody 769 or polyclonal to GAPDH. Blots were developed by enhanced chemiluminescence. Quantification of the relative amounts of bands C and GAPDH was performed by using NIH ImageJ analysis of scanned films [1].

别名	鲁玛卡托, VRT 826809, VX-809
分子量	452.41
分子式	C24H18F2N2O5
CAS No.	936727-05-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

H2O: <1 mg/mL

Ethanol: 6 mg/mL (13.26 mM)

DMSO: 83 mg/mL (183.5 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Van Goor F, et al. Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809. Proc Natl Acad Sci U S A. 2011 Nov 15;108(46):18843-8. 2. Phuan PW, et al. Synergy-based small-molecule screen using a human lung epithelial cell line yields ΔF508-CFTR correctors that augment VX-809 maximal efficacy. Mol Pharmacol. 2014 Jul;86(1):42-51.

文献引用

1. Sondo E, Cresta F, Pastorino C, et al. The L467F-F508del Complex Allele Hampers Pharmacological Rescue of Mutant CFTR by Elexacaftor/Tezacaftor/Ivacaftor in Cystic Fibrosis Patients: The Value of the Ex Vivo Nasal Epithelial Model to Address Non-Responders to CFTR-Modulating Drugs. International Journal of Molecular Sciences. 2022, 23(6): 3175. 2. Baldassarri M, Zguro K, Tomati V, et al.Gain-and Loss-of-Function CFTR Alleles Are Associated with COVID-19 Clinical Outcomes.Cells.2022, 11(24): 4096. 3. Tomati V, Costa S, Capurro V, et al.Rescue by elexacaftor-tezacaftor-ivacaftor of the G1244E cystic fibrosis mutation's stability and gating defects are dependent on cell background.Journal of Cystic Fibrosis.2022

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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稀释计算器

配液计算器

分子量计算器

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浓度

容积

分子量

浓度 (起始)

容积 (起始)

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容积 (终)

溶液体积

质量

配液浓度

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Lumacaftor 936727-05-8 Autophagy Membrane transporter/Ion channel CFTR 鲁玛卡托 VRT 826809 VX809 VX 809 VRT826809 Cystic fibrosis transmembrane conductance regulator Inhibitor VRT-826809 VX-809 inhibit inhibitor

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Lumacaftor

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溶解度

参考文献

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剂量换算

体内实验配液计算器

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