Balaglitazone is an agonist of peroxisome proliferator-activated receptor (PPAR) γ, with an EC50 of 1.351 μM for human PPARγ. Balaglitazone reverses multidrug resistance (MDR) in K562/DOX cells. Balaglitazone (25 µM) increases Rh123 accumulation in K562/DOX cells, but does not increases MFI in K562 cells. Balaglitazone downregulates P-gp expression in K562/DOX cells, and such effects are via upregulation of PTEN in K562/DOX cells, and be abolished by PTEN inhibition.
In vivo, Balaglitazone (3 mg/kg, p.o.) shows antihyperglycaemic activity in fully diabetic and insulin resistant db/db mice, and is more potent than the full PPARγ agonist rosiglitazone. Balaglitazone (10 mg/kg, p.o.) suppresses overall glucose, decreases insulin levels, and increases bodyweight in male diet-induced obese rats, and such effects are equal to that of 30 mg/kg pioglitazone.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL|
Balaglitazone reverses P-glycoprotein-mediated multidrug resistance via upregulation of PTEN in a PPARγ-dependent manner in leukemia cells.
Yousefi B, et al. Tumour Biol. 2017 Oct;39(10):1010428317716501. PMID: 28978268.
Dissociation of antihyperglycaemic and adverse effects of partial perioxisome proliferator-activated receptor (PPAR-gamma) agonist balaglitazone.
Larsen PJ, et al. Eur J Pharmacol. 2008 Oct 31;596(1-3):173-9. PMID: 18761337.
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