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, administered orally at doses ranging from 1 to 3 mg/kg, effectively reduces the postprandial elevation in plasma glucose levels and decreases the glucose area under the curve (AUCglucose) for up to five hours following a meal [2]. This dose-dependent suppression of AUCglucose was observed in an animal model involving pregnant Wistar rats aged 12 weeks, with dosages administered at 0.3 mg/kg, 1 mg/kg, and 3 mg/kg [2].