Mitiglinide (KAD-1229) is an insulinotropic agent that is an ATP-sensitive K + (K ATP ) channel antagonist. Mitiglinide is highly specific to the Kir6.2/SUR1 complex (the pancreatic beta-cell K ATP channel). Mitiglinide is able to be used for the research of type 2 diabetes [1] [2].

In COS-1 cells, Mitiglinide inhibits the Kir6.2/SUR1 channel currents in a dose-dependent manner (IC 50 of 100 nM) but does not significantly inhibit either Kir6.2/SUR2A or Kir6.2/SUR2B channel currents even at high doses (over 10 μM) [1].

Mitiglinide (1-3 mg/kg; p.o.) inhibits the increase of plasma glucose levels seen after a meal load and the area under the curve for plasma glucose levels (AUCglucose) up to 5 h after the meal load [2]. Animal Model: Pregnant Wistar rats (12 weeks) [2] Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg Administration: Oral administration Result: Dose-dependently suppressed AUC glucose levels.