产品描述:
Arhalofenate is an orally bioavailable prodrug form of the free acid form of a peroxisome proliferator-activated receptor γ (PPARγ) partial agonist.{57707} It is converted to the active free acid form by nonspecific serum esterases. Arhalofenate has weak PPARγ transactivation activity in a reporter assay but strong transrepression activity, reducing LPS-induced chemokine (C-C motif) ligand 2 (CCL2) secretion in isolated mouse peritoneal macrophages. It reduces fasting plasma glucose levels in ob/ob mouse and Zucker diabetic fatty (ZDF) rat models of type 2 diabetes when administered at doses of 125 and 100 mg/kg, respectively. It also decreases fasting free fatty acid, triglyceride, and cholesterol levels in ZDF rats without increasing body weight when administered at a dose of 100 mg/kg.{57708} Arhalofenate (250 mg/kg) prevents leukocyte and neutrophil infiltration and IL-1β, IL-6, and chemokine (C-X-C motif) ligand 1 (CXCL1) production in air pouch fluid in a mouse model of gout.{57709}