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Balaglitazone

Cat. No. M9496
Balaglitazone Structure
Synonym:

DRF-2593; NN-2344; NNC-610645

Size Price Availability Quantity
10mg USD 340 In stock
25mg USD 640 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 395.43
Formula C20H17N3O4S
CAS Number 199113-98-9
Purity >98.5%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Balaglitazone, DRF-2593; NN-2344; NNC-610645 supplier, PPAR, inhibitors

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