Cayman Chemical | GW 9662 | Description (CAS 22978-25-2)

70785 GW 9662

(CAS 22978-25-2)

Click image to enlarge

• See below for pricing and ordering

• See analysis tools

• See more Nuclear Receptors; PPAR; Receptor Antagonist; Atherosclerosis; Endocrinology; Metabolism

Chemical structure definitions are available for many Cayman products. See Chemical Structure Database for details.

The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.^1,2 Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.³ There are many PPARγ agonists, including 15-deoxy-Δ^12,14-prostaglandin J₂ and azelaoyl PAF, which are naturally derived.^4,5 However, only a few antagonists have been reported.⁶ GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.⁶ It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.⁷

1 Willson, T.M., Cobb, J.E., Cowan, D.J., et al. The structure-activity relationship between peroxisome proliferator-activated receptor γ agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem 39 665-668 (1996).

2 Maxey, K.M., Hessler, E., MacDonald, J., et al. The nature and composition of 15-deoxy-Δ^12,14-PGJ₂. Prostaglandins and Other Lipid Mediators 62 15-21 (2000).

3 Wright, H.M., Clish, C.B., Mikami, T., et al. A synthetic antagonist for the peroxisome proliferator-activated receptor γ inhibits adipocyte differentiation. J Biol Chem 275 1873-1877 (2000).

4 Lehmann, J.M., Moore, L.B., Smith-Oliver, T.A., et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-acivated receptor γ (PPARγ). J Biol Chem 270 12953-12956 (1995).

5 Cantello, B.C.C., Cawthorne, M.A., Cottam, G.P., et al. [[ω-(Heterocyclylamino)alkoxy]benzyl]-2,4-thiazolidinediones as potent antihyperglycemic agents. J Med Chem 37 3977-3985 (1994).

6 Davies, S.S., Pontsler, A.V., Marathe, G.K., et al. Oxidized alkyl phospholipids are specific, high affinity peroxisome proliferator-activated receptor γ ligands and agonists. J Biol Chem 276 16015-16023 (2001).

7 Bendixen, A.C., Shevde, N.K., Dienger, K.M., et al. IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor γ1. Proc Natl Acad Sci USA 98 2443-2448 (2001).

	Download Product Insert 136 Kb PDF
	Download Material Safety Data Sheet (MSDS) 18 Kb PDF
	Printer-friendly version of this page small PDF (usually less than 100 Kb)
	• US Letter paper 8½″ × 11″
	• A4 paper 21cm × 29.7cm

Purchase 70785 GW 9662

Pricing is for North America only. Other customers should contact a distributor in their region.

This product is also available to buy in bulk quantities. Please contact our Sales Department for a quote or to purchase.

Cayman strives to be a reliable biochemical reagent vendor by providing the best possible products and services. To ask for assistance with one of our products please contact our Technical Help staff.

Warning This product is not for human or veterinary use.

Pricing updated 2010-03-15.
Prices are subject to change without notice.

Related Products

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.