{"id":3034,"date":"2018-04-07T08:32:48","date_gmt":"2018-04-07T08:32:48","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/technical-note\/mdck-wt-mdr1-permeability\/"},"modified":"2025-11-26T14:17:20","modified_gmt":"2025-11-26T14:17:20","slug":"mdck-wt-mdr1-permeability","status":"publish","type":"technical-note","link":"https:\/\/www.sygnaturediscovery.com\/fr\/technical-note\/mdck-wt-mdr1-permeability\/","title":{"rendered":"MDCK-WT\/MDR1 Permeability"},"content":{"rendered":"<p>Wild-type MDCK (Madin-Darby canine kidney) cells, when transfected with either the Multidrug Resistance gene-1 (MDR1; P-gp) or Breast Cancer Resistance gene (BCRP), are used as a model of brain penetration and to understand the impact of drug transporters on drug uptake into the brain. When cultured as a monolayer, MDCK cells differentiate to form tight junctions between cells that mimic the blood-brain barrier.<\/p>\n<p>Differentiated and polarized MDCK cells, wild-type and MDR1 (BCRP transfected\u00a0cells are also available), are plated on a 96-transwell permeable system as a single monolayer to allow for automated high throughput screening of compounds. Drug transport is assessed in both directions (apical to basolateral (A-B) and basolateral to apical (B-A)) across the cell monolayer (Figure 1). The buffer used for the assay does not include HEPES, to minimise the inhibitory effect on uptake transporters (Luo\u00a0<em>et al<\/em>., 2010).<\/p>\n<p>Test compound concentrations are quantified using a calibration curve following analysis by LC-MS\/MS, and the apparent permeability coefficient (Papp) and efflux ratio of the compound across the monolayer are calculated. The efflux ratio is used as an indicator of active efflux.<\/p>\n<p>&nbsp;<\/p>\n<p><a href=\"https:\/\/www.sygnaturediscovery.com\/publications\/technical-notes\/caco-2-permeability\/\"><img loading=\"lazy\" decoding=\"async\" class=\"wp-image-1743 aligncenter\" src=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Figure1.jpg\" alt=\"\" width=\"539\" height=\"241\" \/><\/a><\/p>\n<p style=\"text-align: center;\"><strong>Figure 1<\/strong> The schematic illustrates the Transwell of PrediPort\u2122-WT\/MDR1\/BCRP Multiwell Insert<\/p>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":3016,"template":"","category":[1],"resource_tag":[],"class_list":["post-3034","technical-note","type-technical-note","status-publish","has-post-thumbnail","hentry","category-uncategorized"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v27.4 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>MDCK-WT\/MDR1 Permeability - Sygnature<\/title>\n<meta name=\"description\" content=\"MDCK Cell Models: Uncover Brain Penetration &amp; Drug Transport. 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