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475479-34-6

475479-34-6 structure
475479-34-6 structure
  • Name: Aleglitazar
  • Chemical Name: (2S)-2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]propanoic acid
  • CAS Number: 475479-34-6
  • Molecular Formula: C24H23NO5S
  • Molecular Weight: 437.50800
  • Catalog: Research Areas Metabolic Disease
  • Create Date: 2018-07-19 21:36:44
  • Modify Date: 2024-01-02 13:44:26
  • Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)Target: PPARα/γAleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARα and PPARγ. Aleglitazar is being developed for the treatment of type II diabetes; It is currently in phase III clinical trials. In preliminary clinical studies, Aleglitazar has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. Aleglitazar has beneficial effects on both lipid and glucose parameters and may have a therapeutic role in modifying cardiovascular risk factors and improving glycemic control in patients with T2DM. Aleglitazar combines the lipid benefits of fibrates and the insulin-sensitizing benefits of thiazolidinediones.

Name (2S)-2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]propanoic acid
Synonyms UNII-41T4OAG59U
R-1439
Aleglitazar
Description Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)Target: PPARα/γAleglitazar (R1439) is a dual peroxisome proliferator-activated receptor (PPAR) agonist, with affinity to PPARα and PPARγ. Aleglitazar is being developed for the treatment of type II diabetes; It is currently in phase III clinical trials. In preliminary clinical studies, Aleglitazar has been demonstrated to improve hyperglycemia and dyslipidemia in patients with type 2 diabetes mellitus. Aleglitazar has beneficial effects on both lipid and glucose parameters and may have a therapeutic role in modifying cardiovascular risk factors and improving glycemic control in patients with T2DM. Aleglitazar combines the lipid benefits of fibrates and the insulin-sensitizing benefits of thiazolidinediones.
Related Catalog
Target

PPARγ:19 nM (IC50)

PPARα:38 nM (IC50)

References

[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.

Density 1.29
Boiling Point 665.151ºC at 760 mmHg
Molecular Formula C24H23NO5S
Molecular Weight 437.50800
Flash Point 356.071ºC
Exact Mass 437.13000
PSA 110.03000
LogP 5.12830
Index of Refraction 1.627
Storage condition 2-8℃

~99%

475479-34-6 structure

475479-34-6

Literature: US2005/70714 A1, ; Page/Page column 10 ;

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475479-34-6 structure

475479-34-6

Literature: US2010/249428 A1, ; Page/Page column 10 ;

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475479-34-6 structure

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Literature: WO2013/181384 A1, ; Paragraph 0069; 0070; 0071; 0072 ;

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475479-34-6 structure

475479-34-6

Literature: US2003/55265 A1, ;