E17241

An inducer of ABCA1 expression, induces the expression of ABCA1 in a reporter assay using HepG2 cells (EC50 = 280 nM), an agonist of PPARs, induces PPAR-mediated gene expression in reporter assays using HepG2 cells expressing PPARgamma, PPARalpha, or PPARdelta (EC50s = 290, 3,900, and 879 nM, respectively), increases the protein levels of ACBA1 in RAW 264.7 cells but not in the presence of siRNA targeting mRNA encoding PKCzeta, increases cholesterol efflux in RAW 264.7 cells at 0.4, 2, or 10 µM, reduces plasma levels of cholesterol, ALT, and AST and hepatic levels of cholesterol and triglycerides, as well as decreases aortic lesion area in an ApoE-/- mouse model of atherosclerosis when administered at a dose of 25 mg/kg, decreases plasma glucose levels and body weight in KKAy diabetic mice fed a HFHG diet at 50 mg/kg per day. Formulation: A solid. InChI: InChI=1S/C15H14N2O2S2/c18-12-2-1-7-16-13(12)17-14(19)10-3-5-11(6-4-10)15-20-8-9-21-15/h1-7,15,18H,8-9H2,(H,16,17,19). InChIKey: IOZLWSWLSUBSJM-UHFFFAOYSA-N. SMILES: OC1=CC=CN=C1NC(C(C=C2)=CC=C2C3SCCS3)=O