A selective PPARd agonist that acts as a partial agonist (EC50 = 53 nM) in transactivation assays and as a full agonist (EC50 = 30 nM) in the oxidation of free fatty acid; increases HDL levels

CAY10592 – 1 mg

Brand:
Cayman
CAS:
685139-10-0
Storage:
-20
UN-No:
Non-Hazardous - /

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.{14553,16792} 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.{11379} 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.{15689} 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.{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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SKU: 10012536 - 1 mg Category:

Description

A selective PPARd agonist that acts as a partial agonist (EC50 = 53 nM) in transactivation assays and as a full agonist (EC50 = 30 nM) in the oxidation of free fatty acid; increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity in high fat fed ApoB100/CETP-transgenic mice at a dose of 20 mg/kg

Formal name: 2-[4-[[3,3-bis(4-bromophenyl)-2-propen-1-yl]thio]-2-chlorophenoxy]-acetic acid

Synonyms: 

Molecular weight: 568.7

CAS: 685139-10-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Lipids & Lipoproteins|Lipoproteins||Research Area|Endocrinology & Metabolism|Hormones & Receptors|PPARs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity

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