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Cat. Number
702201117898433
Chemical Name
Pioglitazone
References
Formal Name 5-​[[4-​[2-​(5-​ethyl-​2-​pyridinyl)ethoxy]phenyl]methyl]-​2,​4-​thiazolidinedione
CAS Number 111025-46-8
Molecular Formula C19H20N2O3S
Formula Weight 356.4
Formulation A crystalline solid
Purity >98%
Stability 1 year
Storage -20°C
Shipping Wet ice in continental US; may vary elsewhere

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).

Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J Med Chem 43(4) 528-550 (2000).

Sakamoto, J., Kimura, H., Moriyama, S., et al. Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochem Biophys Res Commun 278 704-711 (2000).

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Description

Thiazolidinediones (TZDs) are a group of structurally related PPARγ agonists with anti-diabetic actions in vivo.1,2 Rosiglitazone (BRL49653) is a prototypical TZD and has served as a reference compound for this class of PPARγ ligands.3 Pioglitazone is a closely related TZD which also selectively activates PPARγ-1. Pioglitazone is about one tenth as potent as rosiglitazone, with an EC50 of about 500-600 nM for both human and mouse PPARγ.4,5 In a transactivation assay using COS-1 cells transfected with full length human PPARα and RXRα, pioglitazone and rosiglitazone exhibit low level activation of PPARα at 1 µM and 5.4- and 4.2-fold activation, respectively, at a concentration of 10 µM.4

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).

4 Sakamoto, J., Kimura, H., Moriyama, S., et al. Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochem Biophys Res Commun 278 704-711 (2000).

5 Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J Med Chem 43(4) 528-550 (2000).

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