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Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.3 nM). It binds to microsomes derived from RINm5F pancreatic β-cells (Kd = 0.3 nM) and inhibits 86Rb+ efflux from intact RINm5 cells with a half-maximal inhibition (K0.5) value of 0.06 nM. Glyburide (5 mg/kg) reduces blood glucose levels and increases the activity of hepatic glutathione-S-transferase (GST) and glucose-6-phosphate dehydrogenase (G6PDH) in a rat model of diabetes induced by streptozotocin . It inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed bone marrow-derived macrophages (BMDMs). Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana. Formulations containing glyburide have been used in the treatment of type 2 diabetes.

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