Glyburide (potassium salt)

Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.3 nM). It binds to microsomes derived from RINm5F pancreatic beta-cells (Kd = 0.3 nM) and inhibits 86Rb+ efflux from intact RINm5 cells with a half-maximal inhibition (K0.5) value of 0.06 nM. Glyburide (5 mg/kg) reduces blood glucose levels and increases the activity of hepatic glutathione-S-transferase (GST) and glucose-6-phosphate dehydrogenase (G6PDH) in a rat model of diabetes induced by streptozotocin (STZ, Cay-13104). It inhibits ATP-induced increases in caspase-1 activation and IL-1beta and IL-18 secretion in a concentration-dependent manner in LPS-primed bone marrow-derived macrophages (BMDMs). Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana. Formulations containing glyburide have been used in the treatment of type 2 diabetes.Formal Name: 5-chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl]-2-methoxy-benzamide, monopotassium salt. CAS Number: 52169-36-5. Synonyms: Glibenclamide. Molecular Formula: C23H27ClN3O5S . K. Formula Weight: 532.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 228 nm. SMILES: COC1=C(C(NCCC2=CC=C(S([N-]C(NC3CCCCC3)=O)(=O)=O)C=C2)=O)C=C(Cl)C=C1.[K+]. InChi Code: InChI=1S/C23H28ClN3O5S.K/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18,/h7-12,15,18H,2-6,13-14H2,1H3,(H3,25,26,27,28,29),/q,+1/p-1. InChi Key: KYWKCYNEBFMDBB-UHFFFAOYSA-M.