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Diazoxide-d3 is intended for use as an internal standard for the quantification of diazoxide 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.

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