{"id":3015,"date":"2018-03-07T11:31:06","date_gmt":"2018-03-07T11:31:06","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/technical-note\/caco-2-permeability\/"},"modified":"2025-11-28T14:23:55","modified_gmt":"2025-11-28T14:23:55","slug":"caco-2-permeability","status":"publish","type":"technical-note","link":"https:\/\/www.sygnaturediscovery.com\/fr\/technical-note\/caco-2-permeability\/","title":{"rendered":"Caco-2 Permeability"},"content":{"rendered":"<p>The human colon epithelial cancer cell line, Caco-2, is used as a model of human intestinal absorption of drugs. This model is suitable to test compound suitability for oral dosing, predict intestinal permeability and investigate drug efflux.<\/p>\n<p>When cultured as a monolayer, Caco-2 cells differentiate to form tight junctions between cells to serve as a model of passive diffusion of compounds across the monolayer. Various uptake and efflux transporters are expressed in Caco-2 cells.<\/p>\n<p>Differentiated and polarized Caco-2 cells (21-day system) 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><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-1743\" src=\"https:\/\/www.sygnaturediscovery.com\/wp-content\/uploads\/2025\/11\/Figure1.jpg\" alt=\"\" width=\"407\" height=\"182\"><\/p>\n<p style=\"text-align: center;\"><strong>Figure 1<\/strong> Schematic illustrating the Transwell of CacoReady\u2122 Multiwell Insert<\/p>\n","protected":false},"excerpt":{"rendered":"<p>The human colon epithelial cancer cell line, Caco-2, is used as a model of human intestinal absorption of drugs. This model is suitable to test compound suitability for oral dosing, predict intestinal permeability and investigate drug efflux.<\/p>\n","protected":false},"featured_media":3016,"template":"","category":[1],"resource_tag":[],"class_list":["post-3015","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 v27.5 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Caco-2 Permeability - Sygnature<\/title>\n<meta name=\"description\" content=\"Caco-2, is used as a model of human intestinal absorption of drugs; suitable to test compound suitability for oral dosing, predict ...\" \/>\n<meta name=\"robots\" content=\"noindex, follow\" \/>\n<meta property=\"og:locale\" content=\"fr_CA\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Caco-2 Permeability - Sygnature\" \/>\n<meta property=\"og:description\" content=\"Caco-2, is used as a model of human intestinal absorption of drugs; 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