ChemicalBook CAS DataBase List 1266523-09-4

1266523-09-4

Name	Pioglitazone (potassium salt)
CAS	1266523-09-4
Molecular Formula	C19H21KN2O3S
Molecular Weight	396.55
MOL File	1266523-09-4.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMF: 30 mg/ml; DMSO: 10 mg/ml; Ethanol: 10 mg/ml
form	A crystalline solid

Hazard Information

Uses

Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research[2][3][4].

in vivo

Pioglitazone potassium (oral gavage, 10 or 30 mg/kg, once daily, 14 days) can induce improvements in insulin resistance and diabetes that may be lipocalin-dependent in the liver but not in skeletal muscle^[3].
Pioglitazone potassium (oral gavage, 10 mg/kg, once daily, 4 weeks) can significantly reduce body weight (BW), cardiac hypertrophy, elevated blood glucose levels and improve the associated dyslipidemia^[4].

Animal Model:	ob/ob and adipo^-/- ob/ob mice with a C57Bl/6 background^[3]
Dosage:	10 or 30 mg/kg
Administration:	Oral gavage; once daily; 14 days
Result:	Showed no changes of serum-free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob and adipo^-/- ob/ob C57BL/6 mice at 10 mg/kg but significantly reduced to a similar degree at 30 mg/kg. Also showed no changes of expressions of TNFα and resistin in adipose tissues of ob/ob and adipo^-/- ob/ob mice at 10 mg/kg but decreased at 30 mg/kg.

Animal Model:	Male Wistar albino rats^[4]
Dosage:	10 mg/kg
Administration:	Oral gavage; once daily; 4 weeks
Result:	Decreased the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB), TGF-β1 gene expression and regulated the expression of MMP-2/TIMP-2 system.

IC 50

mouse PPARγ: 0.99 μM (EC₅₀); h-PPARγ: 0.93 μM (EC₅₀); hPPARδ: 43 μM (EC₅₀); hPPARα: 100 μM (EC₅₀); mouse PPARα: 100 μM (EC₅₀)

storage

Store at -20°C

References

[1] Kenji Kuwabara, et al. A novel selective peroxisome proliferator-activated receptor alpha agonist,2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose levels and modifies lipoprotein profiles in KK-Ay mice. J Pharmacol Exp Ther. 2004 Jun;309(3):970-7. DOI:10.1124/jpet.103.064659
[2] A Puddu, et al. Pioglitazone attenuates the detrimental effects of advanced glycation end-products in the pancreatic beta cell line HIT-T15. Regul Pept. 2012 Aug 20;177(1-3):79-84. DOI:10.1016/j.regpep.2012.05.089
[3] Naoto Kubota, et al. Pioglitazone ameliorates insulin resistance and diabetes by both adiponectin-dependent and -independent pathways. J Biol Chem. 2006 Mar 31;281(13):8748-55. DOI:10.1074/jbc.M505649200
[4] Rania A Elrashidy, et al. Pioglitazone attenuates cardiac fibrosis and hypertrophy in a rat model of diabetic nephropathy. J Cardiovasc Pharmacol Ther. 2012 Sep;17(3):324-33. DOI:10.1177/1074248411431581

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