Chemical Name: 4-(2-Chloro-4-fluorophenyl)-1,4,5,7-tetrahydro-3-methyl-1-(9H-purin-6-yl)-6H-pyrazolo[3,4-b]pyridin-6-one
Biological ActivityPotent and selective GPR39 agonist (IC50 values are 280 and 9 nM in the absence and presence of Zn2+, respectively). Exhibits no significant activity against a panel of 165 other GPCRs. Inhibits the release of ghrelin and somatostatin from primary gastric mucosa cells in vitro. Cell permeable and orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Model-based discovery of synthetic agonists for the Zn2+-sensing G-protein-coupled receptor 39 (GPR39) reveals novel biological functions.
Frimurer et al.
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