A SUR1/Kir6.2 inhibitor (IC50 = 4 nM); selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 3 and 5 µM

Mitiglinide (calcium salt) – 100 mg

Brand:
Cayman
CAS:
145525-41-3
Storage:
-20
UN-No:
Non-Hazardous - /

Mitiglinide is an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4 nM).{54249} It is selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 3 and 5 µM, respectively). Mitiglinide induces insulin release in HIT-T15 insulinoma cells and isolated mouse pancreatic islets when used at a concentration of 100 µM.{54250} Oral administration of mitiglinide (1, 3, and 10 mg/kg) increases postprandial plasma insulin levels and inhibits postprandial increases in plasma glucose levels in a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104).{54251}  

 

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Description

A SUR1/Kir6.2 inhibitor (IC50 = 4 nM); selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 3 and 5 µM, respectively); induces insulin release in HIT-T15 insulinoma cells and isolated mouse pancreatic islets at 100 µM; increases postprandial plasma insulin levels and inhibits postprandial increases in plasma glucose levels in an STZ-induced rat model of diabetes

Formal name: (αS,3aR,7aS)-octahydro-γ-oxo-α-(phenylmethyl)-2H-isoindole-2-butanoic acid, hemicalcium salt

Synonyms:  KAD-1229|S21403

Molecular weight: 334.4

CAS: 145525-41-3

Purity: ≥98% (mixture of isomers)

Formulation: A crystalline solid

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