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Diazoxide-d3 is intended for use as an internal standard for the quantification of diazoxide (Item No. 14576) by GC- or LC-MS. Diazoxide is an activator of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = 14.1 µM in a FLIPR assay using HEK293 cells).1 It also activates SUR2A/Kir6.2 and SUR2B/Kir6.2 channels in HEK293T cells in a patch-clamp assay when used at concentrations of 30 and 300 µM.2 Diazoxide inhibits glucose-induced insulin release from isolated rat pancreatic β cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 µM, respectively).3 It reduces mean arterial pressure and cerebral blood flow in spontaneously hypertensive rats when administered intravenously as a 5 mg/kg bolus dose.4 Diazoxide (50 mg/kg, i.p.) increases blood glucose levels in mice.5 Formulations containing diazoxide have been used in the treatment of hypoglycemia.
WARNING This product is not for human or veterinary use.
1. Pharmacology of human sulphonylurea receptor SUR1 and inward rectifier K+ channel Kir6.2 combination expressed in HEK-
2. C-
3. Toward tissue-
4. Effect of diazoxide-
5. Effect of single dose administration of diuretics on the blood sugar of alloxan-