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Synonyms: Fulyzaq® | SP-303
crofelemer is an approved drug (FDA (2012))
Compound class:
Natural product or derivative
Comment: Crofelemer is an oligomeric proanthocyanidin extracted from Croton lechleri, a South American flowering tree of the Euphorbiaceae (or spurges). We do not show a chemical structure for this complex molecule, but [2] shows a putative chemical structure.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖
View more information in the IUPHAR Pharmacology Education Project: crofelemer |
| 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 ion channels | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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