Muraglitazar is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ (ECs = 0.32 and 0.11 μM, respectively). It is selective for PPARα/γ over other nuclear receptors, including PPARδ, RXRα, RARs, estrogen receptor α (ERα), ERβ, androgen receptor (AR), and progesterone receptor (PR). Muraglitazar (50 μM) reduces the size of lipid droplets in oleic acid-treated HepaRG human hepatocytes. It reduces plasma levels of glucose, triglycerides, free fatty acids, and insulin by 54, 33, 62, and 48%, respectively, in db/db mice when administered at a dose of 10 mg/kg per day. Muraglitazar (10 mg/kg per day) reduces plasma levels of glucose, triglycerides, and cholesterol in diet-induced obese mice. Muraglitazar also inhibits LPS-induced increases in nitric oxide (NO) production and IL-6, TNF-α, and inducible nitric oxide synthase (iNOS) protein levels in J774 murine macrophages in a concentration-dependent manner. It inhibits carrageenan-induced paw edema in mice when administered at doses ranging from 12.5 to 50 mg/kg.