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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.
| Molecular Weight | 395.43 |
| Formula | C20H17N3O4S |
| CAS Number | 199113-98-9 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PPAR Products |
|---|
| WY 14643 (Pirinixic Acid)
WY 14643 (Pirinixic Acid) is a potent and selective, peroxisome proliferator-activated receptor-α (PPARα) agonist. |
| Rosiglitazone
Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50=60 nM, Kd=40 nM). Rosiglitazone is an TRPC5 activator (EC50=30 μM) and TRPM3 inhibitor. |
| GSK 3787
GSK3787 is an orally available selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6). |
| Rosiglitazone maleate
Rosiglitazone maleate (Avandia) is a potent and selective PPARγ ligand that binds to the PPARγ ligand-binding domain with a Kd value of 43 nM. |
| Ciprofibrate
Ciprofibrate is a peroxisome proliferator-activated receptor α (PPARα) agonist. |
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