Diazoxide

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). 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. Diazoxide inhibits glucose-induced insulin release from isolated rat pancreatic beta cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 µM, respectively). It reduces mean arterial pressure and cerebral blood flow in spontaneously hypertensive rats when administered intravenously as a 5 mg/kg bolus dose. Diazoxide (50 mg/kg, i.p.) increases blood glucose levels in mice. Formulations containing diazoxide have been used in the treatment of hypoglycemia.Formal Name: 7-chloro-3-methyl-1,1-dioxide-2H-1,2,4-benzothiadiazine. CAS Number: 364-98-7. Synonyms: NSC 64198, NSC 76130, SRG 95213. Molecular Formula: C8H7ClN2O2S. Formula Weight: 230.7. Purity: >99%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. lambdamax: 267 nm. SMILES: ClC1=CC=C2C(S(NC(C)=N2)(=O)=O)=C1. InChi Code: InChI=1S/C8H7ClN2O2S/c1-5-10-7-3-2-6(9)4-8(7)14(12,13)11-5/h2-4H,1H3,(H,10,11). InChi Key: GDLBFKVLRPITMI-UHFFFAOYSA-N.