Multidrug Efflux Transporter (MDR1/P-gp) Ligand Screening Kit
货号：
K507-100 基本售价：
4320.5 元 规格：
100Assays
产品信息
概述| 货号 | K507-100 |
| 描述 | P-glycoprotein (P-gp, Multidrug Resistance Protein 1 (MDR1), EC 3.6.3.44) is a member of the ATP-binding cassette (ABC) ATPase superfamily of transmembrane transporter proteins. P-gp has an extremely broad substrate specificity and is capable of transporting a vast array of neutral and anionic lipophilic molecules. P-gp strongly affects the oral absorption, tissue distribution and excretion of many drugs and prevents certain lipophilic drugs from penetrating the blood brain barrier. Overexpression of P-gp confers tumor cells with resistance to chemically and pharmacologically distinct chemotherapeutic drugs (such as doxorubicin, vincristine and paclitaxel) by actively pumping them out of cells. Induction of P-gp expression is a frequent cause of treatment failure and tumor-targeted delivery of P-gp inhibitors is being investigated as a strategy for overcoming chemotherapy resistance. BioVision’s MDR1/P-gp Ligand Screening Kit is designed for rapidly screening test compounds for modulation of efflux transporter activity in MDR1-expressing cell lines. The assay uses a lipophilic non-fluorescent P-gp substrate that readily diffuses through the plasma membrane, where it is hydrolyzed to an active fluorophore by cytosolic esterases. The resulting hydrophilic fluorophore is neither membrane permeable nor a substrate for P-gp, hence it remains trapped inside the cell. In MDR1-expressing cell lines, the lipophilic pro-fluorophore is continuously extruded from the cytosol by P-gp, leading to a low intracellular fluorescence. Inhibition of P-gp-mediated efflux by a test compound leads to increased intracellular fluorescence. Specific transporter activity is quantified by comparison with fluorescence accumulated in the presence and absence of a saturating concentration of the included selective P-gp inhibitor. The assay is highly sensitive, has a simple no-wash protocol and is high-throughput adaptable. The kit contains a complete set of reagents sufficient for performing 100 reactions in a 96-well plate format. |
| 同种亚型 | Rabbit IgG |
| 来源宿主 | Rabbit |
性能| 供应商 | Biovision |
| 检测类型 | Detection method- Fluorescence (Ex/Em = 488/532 nm) • Species reactivity - N/A• Applications - Screening/studying/characterizing MDR1/P-gp Inhibitors |
| 产品特色 | • Simple method to screen P-gp inhibitors• High-throughput adaptable• Includes Inhibitor Control, Verapamil |
| 试剂盒组分 | • Efflux Assay Buffer• Fluorogenic P-gp Substrate• P-gp Inhibitor (Verapamil) |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
