AZ876

AZ876 is a selective, orally active agonist of liver X receptor (LXRα/β) (K_i=0.007 μM [LXRα, human], 0.011 μM [LXRβ, human]. AZ876 induces the expression of target genes such as ABCA1 and ABCG1, promotes reverse cholesterol transport (RCT) and regulates lipid metabolism and anti-inflammatory effects. AZ876 increases cardiac polyunsaturated fatty acid levels, reduces myocardial fibrosis, and reduces lesion area and monocyte adhesion in atherosclerosis models. AZ876 can be used in cardiovascular disease research, such as preventing and treating β-adrenergic-induced cardiac diastolic dysfunction and inhibiting the progression of atherosclerosis^[1][2]. In Vitro:AZ876 (10 nM; 6-48 h) induces the expression of LXR target genes (such as SCD2, ELOVL5, FADS2) in HL-1 cardiomyocytes in a time-dependent manner^[1]. In Vivo:AZ876 (20 μmol/kg; oral; once daily; 3 weeks) significantly reduces lesion area, decreases monocyte adhesion, increases cardiac polyunsaturated fatty acid levels, and improves cardiac function in a C57BL/6 mouse model of atherosclerosis^[1].