A sulfonylurea; an inhibitor of SUR1 linked to Kir6.2 (IC50 = 4.3 nM); binds to RINm5F microsomes (Kd = 0.3 nM); inhibits 86Rb+ efflux from intact RINm5 cells (K0.5 = 0.06 nM); reduces blood glucose levels and increases the activity of hepatic GST and G6PDH in an STZ-induced rat model of diabetes at 5 mg/kg; inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed BMDMs; reduces lesion growth in mice infected with L. mexicana at 80 mg/ml

Glyburide (potassium salt) – 5 g

Brand:
Cayman
CAS:
52169-36-5
Storage:
-20
UN-No:
Non-Hazardous - /

Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.3 nM).{22674} 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.{22672} 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 (STZ; Item No. 13104).{43282} 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).{22671} Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana.{22673} Formulations containing glyburide have been used in the treatment of type 2 diabetes.  

 

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Description

A sulfonylurea; an inhibitor of SUR1 linked to Kir6.2 (IC50 = 4.3 nM); binds to RINm5F microsomes (Kd = 0.3 nM); inhibits 86Rb+ efflux from intact RINm5 cells (K0.5 = 0.06 nM); reduces blood glucose levels and increases the activity of hepatic GST and G6PDH in an STZ-induced rat model of diabetes at 5 mg/kg; inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed BMDMs; reduces lesion growth in mice infected with L. mexicana at 80 mg/ml

Formal name: 5-chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxy-benzamide, monopotassium salt

Synonyms:  Glibenclamide

Molecular weight: 532.1

CAS: 52169-36-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Antiparasitics|Antiprotozoals||Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Infectious Disease|Parasitic Diseases|Leishmaniasis

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