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Aleglitazar

Catalog No. T14176   CAS 475479-34-6
Synonyms: RO0728804, R1439

Aleglitazar (R1439) (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.

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Aleglitazar Chemical Structure
Aleglitazar, CAS 475479-34-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 258.00
5 mg In stock $ 592.00
10 mg In stock $ 798.00
25 mg In stock $ 1,220.00
50 mg In stock $ 1,650.00
100 mg In stock $ 2,220.00
1 mL * 10 mM (in DMSO) In stock $ 598.00
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Purity: 99.42%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Aleglitazar (R1439) (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.
Targets&IC50 PPARγ:19 nM, PPARα:38 nM
In vitro Aleglitazar exhibits species selectivity with respect to PPARα, with an EC50s of 50 nM, 2.26 µM and 2.34 µM for human PPARα, rat PPARα and mouse PPARα, respectively[1]. Aleglitazar (0.01-40 µM; 12-48 hours) does not significantly increase lactate dehydrogenase (LDH) release at concentrations of 0.1 µM to 20 µM, but significant increases LDH release at concentrations of 30 µM and 40 µM[2]. Aleglitazar (0.01-20 µM; 48 hours) decreases hyperglycaemic conditions (HG, glucose 25 mM)-induced apoptosis, caspase-3 activity and cytochrome-C release[2]. Aleglitazar improves cell viability in cells exposed to hyperglycaemia[2].
In vivo Aleglitazar (0.3-3.0 mg/kg; i.p.; daily; for 7 days) exerts beneficial effects on structural and functional outcomes of mild brain ischemia[3]. Aleglitazar reduces key aspects of microglia activation including NO production, release of proinflammatory cytokines, migration, and phagocytosis[3]. Aleglitazar attenuates inflammatory responses in post-ischemic brain[3].
Synonyms RO0728804, R1439
Molecular Weight 437.51
Formula C24H23NO5S
CAS No. 475479-34-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45mg/mL (102.9mM)

TargetMolReferences and Literature

1. Bénardeau A, Verry P, Atzpodien EA, et al. Effects of the dual PPAR-α/γ agonist aleglitazar on glycaemic control and organ protection in the Zucker diabetic fatty rat. Diabetes Obes Metab. 2013 Feb;15(2):164-74. 2. Younk LM, Uhl L, Davis SN. Pharmacokinetics, efficacy and safety of aleglitazar for the treatment of type 2 diabetes with high cardiovascular risk. Expert Opin Drug Metab Toxicol. 2011 Jun;7(6):753-63. 3. Foley-Comer AJ, Young AM, Russell-Yarde F, et al. Aleglitazar, a balanced PPARα/γ agonist, has no clinically relevant pharmacokinetic interaction with high-dose atorvastatin or rosuvastatin. Expert Opin Investig Drugs. 2011 Jan;20(1):3-12. 4. Cavender MA, Lincoff AM. Therapeutic potential of aleglitazar, a new dual PPAR-α/γ agonist: implications for cardiovascular disease in patients with diabetes mellitus. Am J Cardiovasc Drugs. 2010;10(4):209-16. 5. Bénardeau A, Benz J, Binggeli A, et al. Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes. Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Obesity Compound Library Anti-Cancer Compound Library Anti-Breast Cancer Compound Library ReFRAME Related Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Clinical Compound Library Drug Repurposing Compound Library

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Keywords

Aleglitazar 475479-34-6 DNA Damage/DNA Repair Metabolism PPAR RO0728804 R1439 RO-0728804 RO 0728804 R-1439 R 1439 inhibitor inhibit

 

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