E17241

E17241 is an inducer of the expression of ABCA1, the gene encoding ATP-binding cassette transporter 1; subfamily A (ABCA1).¹ It induces the expression of ABCA1 in a reporter assay using HepG2 cells (EC₅₀ = 280 nM). E17241 is also an agonist of peroxisome proliferator-activated receptors (PPARs).² It induces PPAR-mediated gene expression in reporter assays using HepG2 cells expressing PPARγ, PPARα, or PPARδ (EC₅₀s = 290, 3,900, and 879 nM, respectively). It increases the protein levels of ACBA1 in RAW 264.7 macrophages but not in the presence of siRNA targeting mRNA encoding PKCζ.¹ E17241 (0.4, 2, or 10 µM) increases cholesterol efflux in RAW 264.7 cells. It reduces plasma levels of cholesterol, alanine transaminase (ALT), and aspartate aminotransferase (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. E17241 (50 mg/kg per day) decreases plasma glucose levels and body weight in KKAy diabetic mice fed a high-fat and high-glucose (HFHG) diet.²

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1. Xu, Y., Liu, C., Hang, X., et al. E17241 as a novel ABCA1 (ATP-binding cassette transporter A₁) upregulator ameliorates atherosclerosis in mice. Arterioscler. Thromb. Vasc. Biol. 41(6), e284-e298 (2021).

2. Sheng, R., Li, Y., Wu, Y., et al. A pan-PPAR agonist E17241 ameliorates hyperglycemia and diabetic dyslipidemia in KKA^y mice via up-regulating ABCA1 in islet, liver, and white adipose tissue. Biomed. Pharmacother. 172, 116200 (2024).