GW 9662

The peroxisome proliferator-activated receptor gamma (PPARgamma) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARgamma agonists with antidiabetic actions in vivo. Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class. There are many PPARgamma agonists, including 15-deoxy-.DELTA.12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived. However, only a few antagonists have been reported. GW 9662 blocks the PPARgamma-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM. It is therefore a much more potent antagonist than BADGE, which is another reported PPARgamma antagonist.. Formulation: A crystalline solid. InChI: InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17). InChIKey: DNTSIBUQMRRYIU-UHFFFAOYSA-N. SMILES: O=C(C1=CC([N+]([O-])=O)=CC=C1Cl)N([H])C2=CC=CC=C2