Fructose-1,6-bisphosphatase-1 Inhibitor

Fructose-1,6-bisphosphatase-1 (FBPase-1) is an enzyme that catalyzes the conversion of fructose-1,6-bisphosphate to fructose-6-phosphate, which is one of the rate-limiting steps in gluconeogenesis. Excess hepatic FBPase-1 activity contributes to hyperglycemia in patients. Thus, the development of specific FBPase-1 inhibitors is of great clinical interest for the treatment of patients with type 2 diabetes. FBPase-1 inhibitor is a cell-permeable benzoxazolo-sulfonamide compound that blocks human FBPase-1 enzymatic activity with an IC50 value of 3.4 µM (Ki = 1.1 µM) by competing at the AMP allosteric binding site. It has been shown to block glucose production in rat hepatoma cells that are starved of nutrients with an IC50 value of 6.6 µM.Formal Name: 2,5-dichloro-N-(5-chloro-2-benzoxazolyl)-benzenesulfonamide. CAS Number: 883973-99-7. Synonyms: F1,6BPase-1 Inhibitor, FBP1 Inhibitor, FBPase-1 Inhibitor. Molecular Formula: C13H7Cl3N2O3S. Formula Weight: 377.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:6): 0.14 mg/ml, DMSO: 14 mg/ml. lambdamax: 204, 287 nm. SMILES: ClC1=CC=C2C(N=C(NS(C3=C(Cl)C=CC(Cl)=C3)(=O)=O)O2)=C1. InChi Code: InChI=1S/C13H7Cl3N2O3S/c14-7-2-4-11-10(5-7)17-13(21-11)18-22(19,20)12-6-8(15)1-3-9(12)16/h1-6H,(H,17,18). InChi Key: JCXZHFCBNFFHRC-UHFFFAOYSA-N.