MD001 is a dual agonist of peroxisome proliferator-activated receptor alpha (PPARalpha) and PPARgamma.1 It binds to PPARalpha and PPARgamma (Kds = 9.55 and 0.14 µM, respectively) but does not bind to PPARbeta/delta at concentrations up to 500 µM. It increases transcriptional activity of PPARalpha and PPARgamma in a cell-based luciferase reporter assay when used at a concentration of 10 µM. MD001 (10 µM) increases expression of PPARalpha, PPARgamma, and retinoid X receptor (RXR), as well as PPARalpha and PPARgamma target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.
Molekulargewicht:
398.41
CAS Nummer:
[2254605-76-8]
Formel:
C25H18O5
Target-Kategorie:
Others|||PPAR
T35800
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
