Repaglinide
Kir6 blocker / Repaglinide is a blocker of the ATP-sensitive potassium channel Kir6 with hypoglycemic activity.1 Clinically useful antidiabetic agent. It displays 30-fold selectivity for pancreatic Kir6.2/SUR1 over cardiac Kir6.1/SUR2B and Kir6/SUR2A channels.2 Repaglinide displayed neuroprotective effects in Huntington disease3, Parkinson’s disease4, and ALS5 via blockade of the DREAM-ATF6 interaction.
Biochemicals & reagents
135062-02-1
1) Mark and Grell (1997), Hypoglycaemic effects of the novel antidiabetic agent repaglinide in rats and dogs; Br. J. Pharmacol. 121 1597 2) Stephan et al. (2006), Selectivity of repaglinide and glibenclamide for the pancreatic over the cardiovascular K(ATP) channels; Diabetologia 49 2039 3) Naranjo et al. (2016), Activating transcription factor 6 Activating transcription factor 6 derepression mediates neuroprotection in Huntington disease; J. Clin. Invest. 126 627 4) Motawi et al. (2022), Repaglinide Elicits a Neuroprotective Effect in Rotenone-Induced Parkin's Disease in Rats: Emphasis on Targeting the DREAM-ER Stress BiP/ATF6/CHOP Trajectory and Activation of Mitophagy; ACS Chem. Neurosci. 14 180 5) Gonzalo-Gobernado et al. (2023), Repaglinide Induces ATF6 Processing and Neuroprotection in Transgenic SOD1G93A Mice; Int. J. Mol. Sci. 24 15783
-20°C
TARGET: Ion channel -- PATHWAY: Cation channel -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Diabetes; Neurodegeneration