Ligand id: 7453

Name: crofelemer

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View more information in the IUPHAR Pharmacology Education Project: crofelemer

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Bioactivity Comments
Studies in mouse models report that crofelemer has an inhibitory effect on intestinal cAMP-mediated (active) Cl- and fluid secretion [1]. Patch-clamp analysis of cells stably expressing hCFTR or hANO1, and cAMP and calcium signaling measurements in human colorectal cancer cells (T84 cells) confirm the activity of crofelemer at the proposed human Cl- channels.
Selectivity at Human ion channels
Key to terms and symbols Click column headers to sort
Target Type Action Affinity Units Concentration range (M) Reference
CaCC Inhibitor Inhibition 5.2 pIC50 - 2
pIC50 5.2 (IC50 6.5x10-6 M) [2]
CFTR Inhibitor Inhibition 5.2 pIC50 - 2
pIC50 5.2 (IC50 7x10-6 M) [2]