A SUR1/Kir6.2 channel inhibitor (IC50 = 4.9 µM); selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 85 and 88 µM

Tolbutamide – 100 mg

Brand:
Cayman
CAS:
64-77-7
Storage:
-20
UN-No:
Non-Hazardous - /

Tolbutamide is an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.9 µM).{34125} It is selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 85 and 88 µM, respectively). Tolbutamide increases glucose-induced insulin secretion and calcium influx in isolated mouse pancreatic islets.{54189} In vivo, tolbutamide (80 mg/kg) reduces blood glucose levels in a mouse model of diabetes induced by streptozotocin (STZ; Item No. 13104).{54190} Formulations containing tolbutamide have been used in the treatment of type 2 diabetes.  

 

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Description

A SUR1/Kir6.2 channel inhibitor (IC50 = 4.9 µM); selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 85 and 88 µM, respectively); increases glucose-induced insulin secretion and calcium influx in isolated mouse pancreatic islets; reduces blood glucose levels in a mouse model of STZ-induced diabetes at 80 mg/kg

Formal name: N-[(butylamino)carbonyl]-4-methyl-benzenesulfonamide

Synonyms:  D 860|NSC 23813|NSC 87833|U-2043

Molecular weight: 270.3

CAS: 64-77-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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