Balaglitazone

• CAT Number: I002528
• CAS Number: 199113-98-9
• Molecular Formula: C20H17N3O4S
• Molecular Weight: 395.43
• Purity: ≥95%
• Target: PPAR
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C

Balaglitazone (DRF-2593; NN-2344) is a novel partial agonist of PPAR-γ.IC50 Value:Target: PPARγin vitro: The Rs for the separations were 3.5 for balaglitazone enantiomers, 3.5 for pioglitazone enantiomers, and 3.7 for rosiglitazone. The squared correlation coefficients (r2) were found to be 0.999 for all three compounds [1].in vivo: Balaglitazone treated groups shown significantly reduce of HbA1c (%), FSG (mmol/L), postprandial glucose as comparison to pioglitazone. Balaglitazone 10 mg and 20 mg show the similar magnitudes of the effects which comparable to the effects seen in the pioglitazone 45 mg group. The incidence of fluid retention and fat accumulation fewer than those observed with pioglitazone 45 mg [2]. Sixty male dio induced obese rats were divided into five categories: vehicle, pioglitazone 10 mg/kg, pioglitazone 30 mg/kg, balaglitazone 5 mg/kg, balaglitazone 10 mg/kg. At day -7, 21 and 42 fasting serum samples were collected and whole body tissue composition was evaluated by MR scanning [3].Clinical trial: BALLET: Efficacy and Safety of Treatment With Balaglitazone in Type 2 Diabetes Patients on Stable Insulin Therapy. Phase 3

Reference

1:Balaglitazone: a second generation peroxisome proliferator-activated receptor (PPAR) gamma (γ) agonist. Agrawal R, Jain P, Dikshit SN.Mini Rev Med Chem. 2012 Feb;12(2):87-97. Review. PMID: 22372600 2:Efficacy and safety of the PPARγ partial agonist balaglitazone compared with pioglitazone and placebo: a phase III, randomized, parallel-group study in patients with type 2 diabetes on stable insulin therapy. Henriksen K, Byrjalsen I, Qvist P, Beck-Nielsen H, Hansen G, Riis BJ, Perrild H, Svendsen OL, Gram J, Karsdal MA, Christiansen C; BALLET Trial Investigators..Diabetes Metab Res Rev. 2011 May;27(4):392-401. doi: 10.1002/dmrr.1187. PMID: 21328517 3:A comparison of glycemic control, water retention, and musculoskeletal effects of balaglitazone and pioglitazone in diet-induced obese rats. Henriksen K, Byrjalsen I, Nielsen RH, Madsen AN, Larsen LK, Christiansen C, Beck-Nielsen H, Karsdal MA.Eur J Pharmacol. 2009 Aug 15;616(1-3):340-5. doi: 10.1016/j.ejphar.2009.06.051. Epub 2009 Jul 10. PMID: 19595686 4:Dissociation of antihyperglycaemic and adverse effects of partial perioxisome proliferator-activated receptor (PPAR-gamma) agonist balaglitazone. Larsen PJ, Lykkegaard K, Larsen LK, Fleckner J, Sauerberg P, Wassermann K, Wulff EM.Eur J Pharmacol. 2008 Oct 31;596(1-3):173-9. doi: 10.1016/j.ejphar.2008.08.004. Epub 2008 Aug 16. PMID: 18761337