|
CAY10592 Exclusive
Cayman Chemical Item Number 10012536
Description
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.1↗,2↗ 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.3↗ 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.4↗ 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.4↗ Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases low-density lipoprotein and TG levels, and improves insulin sensitivity.4↗
Formal Name 2-[4-[[3,3-bis(4-bromophenyl)-2-propen-1-yl]thio]-2-chlorophenoxy]-acetic acid
CAS Number 685139-10-0
Molecular Formula C23H17Br2ClO3S
Formula Weight 568.7
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES OC(=O)COc1ccc(SCC=C(c2ccc(Br)cc2)c2ccc(Br)cc2)cc1Cl
InCHI Code 1S/C23H17Br2ClO3S/c24-17-5-1-15(2-6-17)20(16-3-7-18(25)8-4-16)11-12-30-19-9-10-22(21(26)13-19)29-14-23(27)28/h1-11,13H,12,14H2,(H,27,28)
InCHI Key NQIYGYDPRBEUAZ-UHFFFAOYSA-N |