鲁玛卡托|T2595|TargetMol

Lumacaftor
936727-05-8

￥290 1mg 起订

￥663 5mg 起订

￥913 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 鲁玛卡托

英文名称：: Lumacaftor

CAS号：: 936727-05-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.72%

产品类别：: 抑制剂

货号：: T2595

Product Introduction

Bioactivity

名称	Lumacaftor
描述	Lumacaftor (VRT 826809) 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).
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].
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].
体外活性	在培养的源于F508del基因同型突变CF患者的人类支气管上皮细胞中，Lumacaftor（VX-809）改善了F508del-CFTR在内质网的处理，并将氯离子分泌提升到非CF人类支气管上皮细胞的约14%（EC50：81 nM），此水平与携带较少干扰CFTR突变的轻度CF患者相关[1]。VX-809在与细胞共孵育时，不论是在37°C还是27°C，都能在两种细胞系中产生浓度依赖性地增加HRP发光信号，其EC50值相似，约为0.3 μM [2]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 6 mg/mL (13.26 mM) DMSO : 50 mg/mL (110.52 mM)
关键字	VX 809 \| VX809 \| CFTR \| Cystic fibrosis transmembrane conductance regulator \| VRT826809 \| Inhibitor \| VRT-826809 \| Lumacaftor \| inhibit \| Autophagy
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鲁玛卡托|||VX-809|||VRT 826809|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子