The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs), a group of structurally related synthetic agonists with antidiabetic actions in vivo.^1,2 Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class.³ MCC-555 is a structural homolog of rosiglitazone and the other TZDs. MCC-555 binds with about 1/10 the affinity of rosiglitazone to PPARγ.⁴ Despite this, MCC-555 is a more potent antidiabetic agent in whole animal experiments than rosiglitazone and several other prototypic TZDs; the ED₅₀ value in these experiments was 2.7 mg/kg for MCC-555 compared with 7.1 mg/kg for rosiglitazone. MCC-555 is therefore a unique new member of the TZD class and may be useful in differentiating some of the multiple activities attributed to this class of compounds.

≥98%

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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-activated receptor γ (PPARγ). J. Biol. Chem. 270, 12953-12956 (1995).

4.Reginato, M.J.,Bailey, S.T.,Krakow, S.L., et al. A potent antidiabetic thiazolidinedione with unique peroxisome proliferator-activated receptor g -activating properties. The Journal of Biological Chemisty 273, 32679-32684 (1998).