Glyburide (potassium salt)

A sulfonylurea inhibitor of SUR1/Kir6.2

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库存: 现货

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5g

￥1487.00

1190.00

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10g

￥2825.00

2260.00

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货号: ajci71788
CAS: 52169-36-5
别名: Glibenclamide
分子式: C23H28ClN3O5S?K
分子量: 533.1
纯度: >98%
溶解度: DMF: 2 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
储存: Store at -20°C
库存: 现货

Background

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.