71742  Rosiglitazone (potassium salt)

(CAS 316371-84-3)

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• See more Nuclear Receptors; PPAR; Atherosclerosis; Diabetes; Endocrinology

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

Thiazolidinediones are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.1,2 Rosiglitazone is a prototypical thiazolidinedione and has served as a reference compound for this class.3 Rosiglitazone is a potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.3 It activates a luciferase-based PPARγ expression construct with an EC50 of about 1.0 µM.3 Rosiglitazone is active in vivo as a antidiabetic agent in the ob/ob mouse model, and has been used as an oral hypoglycemic agent in the treatment of Type II diabetes in humans for many years. The potassium salt of rosiglitazone is a formulation designed to provide better aqueous solubility than the parent compound.
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  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).
3  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).


Purchase 71742 Rosiglitazone (potassium salt)

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

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Warning This product is not for human or veterinary use.

Pricing updated 2010-03-17.
Prices are subject to change without notice.

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.

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