名称 | CFTR(inh)-172 |
描述 | CFTR(inh)-172 (CFTR Inhibitor-172) is a voltage-independent, selective CFTR inhibitor. |
细胞实验 | Cell toxicity is assayed by the dihydrorhodamine method at 24 hours after cell incubation with 0–1,000 μM inhibitor. (Only for Reference) |
激酶实验 | Screening procedures: Assays are done using a customized screening system consisting of a 3-meter robotic arm, CO2 incubator, plate washer, liquid-handling workstation, bar code reader, delidding station, and two FLUOstar fluorescence platereaders, each equipped with two syringe pumps and HQ500/20X (500 ± 10 nm) excitation and HQ535/30M (535 ± 15 nm) emission filters. The robotic system is integrated using SAMI version 3.3 software modified for two platereaders. Custom software is written in Microsoft VBA (Visual Basic for Applications) to compute base-line–subtracted, normalized fluorescence slopes (giving halide influx rates) from stored data files. The assay is set up by loading the incubator (37°C, 90% humidity, 5% CO2) with 40–60 96-well plates containing the FRT cells, and loading a carousel with 96-well plates containing test compounds and disposable plastic pipette tips. To initiate the assay, each well of a 96-well plate is washed three times in PBS (300 μl/wash), leaving 50 μL PBS. Ten microliters of a CFTR-activating cocktail (5 μM forskolin, 100 μM IBMX, 25 μM apigenin in PBS) is added, and after 5 minutes one test compound (0.5 μL of 1 mM DMSO solution) is added to each well to give 10 μM final concentration. After 10 minutes, 96-well plates are transferred to a platereader for fluorescence assay. Each well is assayed individually for CFTR-mediated I– transport by recording fluorescence continuously (200 ms per point) for 2 seconds (base line) and then for 12 seconds after rapid (<0.5 seconds) addition of 165 μL of isosmolar PBS in which 137 mM Cl– was replaced by I–. |
体外活性 | 6小时20 μg CFTRinh-172完全消除霍乱弧菌诱导的肠液分泌而不影响体内霍乱弧菌的生长. |
体内活性 | CFTRinh-172作为一种选择性的CFTR通道抑制剂,能够完全消除兔泪腺兔腺泡和导管细胞中的Cl-电流。CFTRinh-172时间和剂量依赖性的抑制了CFTR介导的碘离子转运,并且有效抑制多种激动剂或激活剂的CFTR激活。CFTRinh-172不依赖CFTR抑制而诱导ROS产生,线粒体衰竭和NF-κB信号传导途径的激活。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 40.9 mg/mL (100 mM)
|
关键字 | CFTR(inh)-172 | Cystic fibrosis transmembrane conductance regulator | Inhibitor | CFTR(inh) 172 | CFTR(inh)172 | CFTR | inhibit | Autophagy |
相关产品 | Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Hydroxychloroquine | Curcumin | Stavudine | Salicylic acid | Paeonol | Sodium 4-phenylbutyrate |
相关库 | 抑制剂库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 自噬库 | 抗纤维化化合物库 | 离子通道库 | 膜蛋白靶向化合物库 | 表型筛选靶点鉴定库 | 共价抑制剂库 |