Tolbutamide-d9 Chemical Properties

Melting point:

108-111°C

storage temp. 

Refrigerator

solubility 

DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:1): 0.14 mg/ml

form 

A solid

color 

White to off-white

Tolbutamide-d9 Usage And Synthesis

Description

Tolbutamide-d₉ is intended for use as an internal standard for the quantification of tolbutamide by GC- or LC-MS. Tolbutamide is an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel K_ir6.2 (IC₅₀ = 4.9 μM). It is selective for SUR1/K_ir6.2 over SUR2A/K_ir6.2 and SUR2B/K_ir6.2 channels (IC₅₀s = 85 and 88 μM, respectively). Tolbutamide increases glucose-induced insulin secretion and calcium influx in isolated mouse pancreatic islets. In vivo, tolbutamide (80 mg/kg) reduces blood glucose levels in a mouse model of diabetes induced by streptozotocin (STZ; ). Formulations containing tolbutamide have been used in the treatment of type 2 diabetes.

Chemical Properties

White Solid

Uses

Labelled Tolbutamide (T535150). An antidiabetic, used as a hypoglycemic agent in veterinary medicine.

References

[1] PETER PROKS. Sulfonylurea stimulation of insulin secretion.[J]. Diabetes, 2002, 51 Suppl 3: S368-76. DOI: 10.2337/diabetes.51.2007.s368
[2] NOBUYOSHI ISHIYAMA  Jean C H  Magalie A Ravier. Dual mechanism of the potentiation by glucose of insulin secretion induced by arginine and tolbutamide in mouse islets.[J]. American journal of physiology. Endocrinology and metabolism, 2006, 290 3: E540-9. DOI: 10.1152/ajpendo.00032.2005
[3] CLAUS RERUP  Finn T. Streptozotocin- and alloxan-diabetes in mice[J]. European journal of pharmacology, 1969, 7 1: Pages 89-96. DOI: 10.1016/0014-2999(69)90169-1

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