912816-40-1Relevant articles and documents
Design and synthesis of dual peroxisome proliferator-activated receptors γ and δ agonists as novel euglycemic agents with a reduced weight gain profile
Xu, Yanping,Etgen, Garret J.,Broderick, Carol L.,Canada, Emily,Gonzalez, Isabel,Lamar, Jason,Montrose-Rafizadeh, Chahrzad,Oldham, Brian A.,Osborne, John J.,Xie, Chaoyu,Shi, Qing,Winneroski, Leonard L.,York, Jeremy,Yumibe, Nathan,Zink, Richard,Mantlo, Nathan
, p. 5649 - 5652 (2007/10/03)
The design and synthesis of the dual peroxisome proliferator-activated receptor (PPAR) γ/δ agonist (R)-3-{4-[3-(4-chloro-2-phenoxy-phenoxy) -butoxy]-2-ethyl-phenyl}-propionic acid (20) for the treatment of type 2 diabetes and associated dyslipidemia is described. The compound possesses a potent dual hPPAR γ/δ agonist profile (IC50 = 19 nM/4 nM; EC50 = 102 nM/6 nM for hPPARγ and hPPARδ, respectively). In preclinical models, the compound improves insulin sensitivity and reverses diabetic hyperglycemia with less weight gain at a given level of glucose control relative to rosiglitazone.
