CAY10592 |
| カタログ番号GC43180 |
ペルオキシソーム増殖因子活性化受容体（PPAR）α、δ、γは、エネルギー代謝の調節やインスリン感受性およびグルコース代謝に関与するリガンド活性化核内転写因子です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 685139-10-0
Sample solution is provided at 25 µL, 10mM.
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Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ 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. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 µM. 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.
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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