For research use only. Not for therapeutic Use.
Tesaglitazar, also known as AR-H-039242XX; AZ-242; ARH-039242XX, is a PPAR agonist potentially for the treatment of type 2 diabetes. The drug had completed several phase III clinical trials, however in May, 2006 AstraZeneca announced that it had discontinued further development.
| Catalog Number | R008495 |
| CAS Number | 251565-85-2 |
| Synonyms | (αS)-α-Ethoxy-4-[2-[4-[(methylsulfonyl)oxy]phenyl]ethoxy]benzenepropanoic Acid;?(S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic Acid;?AR-H 039242; AR-H 039242XX; AZ 242; Galida; |
| Molecular Formula | C20H24O7S |
| Purity | ≥95% |
| Target | PPAR |
| Solubility | Soluble in DMSO > 10 mM |
| Storage | Desiccate at RT |
| IUPAC Name | (2S)-2-ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl)ethoxy]phenyl]propanoic acid |
| InChI | InChI=1S/C20H24O7S/c1-3-25-19(20(21)22)14-16-6-8-17(9-7-16)26-13-12-15-4-10-18(11-5-15)27-28(2,23)24/h4-11,19H,3,12-14H2,1-2H3,(H,21,22)/t19-/m0/s1 |
| InChIKey | CXGTZJYQWSUFET-IBGZPJMESA-N |
| SMILES | CCOC(CC1=CC=C(C=C1)OCCC2=CC=C(C=C2)OS(=O)(=O)C)C(=O)O |
| Reference | </br>1:PPAR Agonists: II. Fenofibrate and Tesaglitazar Alter Behaviors Related to Voluntary Alcohol Consumption. Blednov YA, Black M, Benavidez JM, Stamatakis EE, Harris RA.Alcohol Clin Exp Res. 2016 Mar;40(3):563-71. doi: 10.1111/acer.12972. Epub 2016 Feb 9. PMID: 26857541 Free PMC Article</br>2:The PPAR α / γ Agonist, Tesaglitazar, Improves Insulin Mediated Switching of Tissue Glucose and Free Fatty Acid Utilization In Vivo in the Obese Zucker Rat. Wallenius K, Kjellstedt A, Thalén P, Löfgren L, Oakes ND.PPAR Res. 2013;2013:305347. doi: 10.1155/2013/305347. Epub 2013 Oct 27. PMID: 24285952 Free PMC Article</br>3:[Peroxisome proliferator-activated receptor α/γ agonist tesaglitazar stabilizes atherosclerotic plaque in diabetic low density lipoprotein receptor knockout mice]. Zhang BC, Li XK, Che WL, Li WM, Hou L, Wei YD, Xu YW.Zhonghua Xin Xue Guan Bing Za Zhi. 2013 Feb;41(2):143-9. Chinese. PMID: 23710746 </br>4:Tesaglitazar ameliorates non-alcoholic fatty liver disease and atherosclerosis development in diabetic low-density lipoprotein receptor-deficient mice. Zhang BC, Li WM, Li XK, Zhu MY, Che WL, Xu YW.Exp Ther Med. 2012 Dec;4(6):987-992. Epub 2012 Sep 17. PMID: 23226761 Free PMC Article</br>5:Tesaglitazar, a dual PPAR-α/γ agonist, hamster carcinogenicity, investigative animal and clinical studies. Lindblom P, Berg AL, Zhang H, Westerberg R, Tugwood J, Lundgren H, Marcusson-Ståhl M, Sjögren N, Blomgren B, Öhman P, Skånberg I, Evans J, Hellmold H.Toxicol Pathol. 2012;40(1):18-32. doi: 10.1177/0192623311429972. Epub 2011 Nov 30. PMID: 22131108 </br>6:Pharmacokinetic-pharmacodynamic assessment of the interrelationships between tesaglitazar exposure and renal function in patients with type 2 diabetes mellitus. Hamrén B, Ohman KP, Svensson MK, Karlsson MO.J Clin Pharmacol. 2012 Sep;52(9):1317-27. doi: 10.1177/0091270011416937. Epub 2011 Nov 1. PMID: 22045829 </br>7:Proliferative and molecular effects of the dual PPARalpha/gamma agonist tesaglitazar in rat adipose tissues: relevance for induction of fibrosarcoma. Glinghammar B, Berg AL, Bjurström S, Stockling K, Blomgren B, Westerberg R, Skånberg I, Hellmold H, Andersson U.Toxicol Pathol. 2011 Feb;39(2):325-36. doi: 10.1177/0192623310394210. Epub 2011 Jan 26. PMID: 21270424 </br>8:Tesaglitazar, a dual peroxisome proliferator-activated receptor agonist (PPAR alpha/gamma), improves metabolic abnormalities and reduces renal injury in obese Zucker rats. Liao J, Soltani Z, Ebenezer P, Isidro-Carrión AA, Zhang R, Asghar A, Aguilar E, Francis J, Hu X, Ferder L, Reisin E.Nephron Exp Nephrol. 2010;114(2):e61-8. doi: 10.1159/000254567. Epub 2009 Nov 4. PMID: 19887847 </br>9:The dual PPARalpha/gamma agonist tesaglitazar blocks progression of pre-existing atherosclerosis in APOE*3Leiden.CETP transgenic mice. van der Hoorn JW, Jukema JW, Havekes LM, Lundholm E, Camejo G, Rensen PC, Princen HM.Br J Pharmacol. 2009 Apr;156(7):1067-75. doi: 10.1111/j.1476-5381.2008.00109.x. Epub 2009 Feb 13. PMID: 19220285 Free PMC Article</br>10:Models for plasma glucose, HbA1c, and hemoglobin interrelationships in patients with type 2 diabetes following tesaglitazar treatment. Hamrén B, Björk E, Sunzel M, Karlsson M.Clin Pharmacol Ther. 2008 Aug;84(2):228-35. doi: 10.1038/clpt.2008.2. Epub 2008 Mar 19. PMID: 18388881 |
