CAY10592

CAY10592

CAT N°: 10012536
Price:

54.00 45.90

Peroxisome proliferator-activated receptors (PPARs) ?, ?, ? are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism.{14553,16792} Pharmacologies of PPAR? receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys.{11379} CAY10592 is a full PPAR? agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties.{15689} In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPAR? agonist (EC50 = 53 nM) with no effect on PPAR? or PPAR? activity up to 30 µM.{15689} Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.{15689}

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