A sulfonylurea inhibitor of SUR1/KIR6.2 (IC50 = 4.2 µM); enhances glucose uptake when used in combination with insulin; reduces glomerulosclerosis and albumin excretion in a rat model of insulin-dependent diabetes (128 mg/kg)

Tolazamide – 50 mg

Brand:
Cayman
CAS:
1156-19-0
Storage:
-20
UN-No:
- /

Tolazamide is a first generation sulfonylurea that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2; IC50 = 4.2 µM in HEK293 cells transfected with the human receptor).{36318} It has no effect on glucose uptake in L6 rat skeletal muscle cells when used at a concentration of 0.6 mg/mL but enhances glucose uptake two-fold when used in combination with insulin.{40738} In vivo, tolazamide (128 mg/kg) reduces glomerulosclerosis and albumin excretion in a rat model of insulin-dependent diabetes induced by streptozotocin (Item No. 13104).{40739} Formulations containing tolazamide have been used in the treatment of type 2 diabetes.  

 

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Description

A sulfonylurea inhibitor of SUR1/KIR6.2 (IC50 = 4.2 µM); enhances glucose uptake when used in combination with insulin; reduces glomerulosclerosis and albumin excretion in a rat model of insulin-dependent diabetes (128 mg/kg)

Formal name: N-[[(hexahydro-1H-azepin-1-yl)amino]carbonyl]-4-methyl-benzenesulfonamide

Synonyms:  NSC 70762

Molecular weight: 311.4

CAS: 1156-19-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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