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Balaglitazone

Catalog No.
A3216
PPAR-γ partial agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$209.00
In stock
5mg
$190.00
In stock
10mg
$290.00
In stock
25mg
$514.00
In stock
50mg
$800.00
In stock

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Background

Balaglitazone is a partial agonist of peroxisome proliferator-activated receptor (PPAR) γ [1].
PPAR plays important roles in the regulation of insulin, triglycerides and lipid metabolism. It is an attractive target for the therapy of Type II Diabetes. Balaglitazone is a partial agonist of PPARγ. The maximum inhibition of PPARγ activity by balaglitazone is 52%. Thus balaglitazone is supposed to have decreased side effects. It has showed potent effects on lowering blood glucose in various animal models [1 and 2].
In a cell-based assay using HEK293 cells transfected with fused PPARγ, treatment of balaglitazone showed sigmoid activation with an EC50 value of 1.35μM. When combined with rosiglitazone, balaglitazone at increased concentrations resulted in the reduction of rosiglitazone’s activity to the level of balaglitazone alone at concentration of 100 nM [3].
In adult male diabetic mice, the oral administration of balaglitazone at increased doses showed more potent and efficacious at lowering glucose levels than rosiglitazone. Balaglitazone also caused reduction of bodyfluid accumulation andfat accumulation without heart enlargement, indicating that it had a better safety profile on the cardiovascular system. Besides that, balaglitazone treatment lasted for 21 days exerted no significant impact on the volumes of blood or plasma. Moreover, balaglitazone was found to have no effect on bone formation at concentrations of up to 10 mg/kg indicating that it was only a partial agonist and led no loss of bone [1 and 2].
References:
[1] Agrawal R, Jain P, Dikshit SN. Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma (γ) agonist. Mini Rev Med Chem. 2012 Feb;12(2):87-97.
[2] Henriksen K, Byrjalsen I, Nielsen RH, Madsen AN, Larsen LK, Christiansen C, Beck-Nielsen H, Karsdal MA. A comparison of glycemic control, water retention, and musculoskeletal effects of balaglitazone and pioglitazone in diet-induced obese rats. Eur J Pharmacol. 2009 Aug 15;616(1-3):340-5.
[3] Larsen PJ, Lykkegaard K, Larsen LK, Fleckner J, Sauerberg P, Wassermann K, Wulff EM. Dissociation of antihyperglycaemic and adverse effects of partial perioxisome proliferator-activated receptor (PPAR-gamma) agonist balaglitazone. Eur J Pharmacol. 2008 Oct 31;596(1-3):173-9.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt395.43
Cas No.199113-98-9
FormulaC20H17N3O4S
SynonymsDRF-2593;NN-2344;DRF2593;NN2344;DRF 2593;NN 2344
Solubility≥15.45 mg/mL in DMSO, ≥2.18 mg/mL in EtOH with ultrasonic and warming,insoluble in H2O
Chemical Name5-(4-((3-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)methoxy)benzyl)thiazolidine-2,4-dione
SDFDownload SDF
Canonical SMILESO=C1C2=CC=CC=C2N=C(COC3=CC=C(CC4C(NC(S4)=O)=O)C=C3)N1C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Balaglitazone (DRF-2593; NN-2344) is a novel partial agonist of PPAR-γ.
Targets PPARγ          
IC50            

Quality Control

Chemical structure

Balaglitazone