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Cat. Number
702012897965178
Chemical Name
Rosiglitazone (potassium salt)
References
Formal Name 5-​[[4-​[2-​(methyl-​2-​pyridinylamino)ethoxy]phenyl]methyl]-​2,​4-​thiazolidinedione,​ monopotassium salt
CAS Number 316371-84-3
Molecular Formula C18H18N3O3S · K
Formula Weight 395.5
Formulation A crystalline solid
Purity >98%
λmax 247 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
CN(CCOC1=CC=C(CC2SC([N-]​C2=O)​=O)​C=C1)​C3=NC=CC=C3.[K+]​

Background Reading

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).

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).

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).

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Description

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).

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