Tesaglitazar
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Hodoodo CAT#: H326990

CAS#: 251565-85-2

Description: 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.

Chemical Structure

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Tesaglitazar
CAS# 251565-85-2
Instruction

Theoretical Analysis

Hodoodo Cat#: H326990
Name: Tesaglitazar
CAS#: 251565-85-2
Chemical Formula: C20H24O7S
Exact Mass: 408.12
Molecular Weight: 408.465
Elemental Analysis: C, 58.81; H, 5.92; O, 27.42; S, 7.85

Price and Availability

Size Price Availability Quantity
10mg USD 350
20mg USD 650
50mg USD 1350
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Synonym: Tesaglitazar; AR-H-039242XX; AZ-242; AZ242; AZ 242; ARH-039242XX; Galida.

IUPAC/Chemical Name: (2S)-2-Ethoxy-3-(4-(2-(4-((methylsulfonyl)oxy)phenyl)ethoxy)phenyl)propanoic acid

InChi Key: CXGTZJYQWSUFET-IBGZPJMESA-N

InChi Code: 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

SMILES Code: O=C(O)[C@@H](OCC)CC1=CC=C(OCCC2=CC=C(OS(=O)(C)=O)C=C2)C=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 408.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Blednov YA, Black M, Benavidez JM, Stamatakis EE, Harris RA. PPAR Agonists: II. Fenofibrate and Tesaglitazar Alter Behaviors Related to Voluntary Alcohol Consumption. Alcohol Clin Exp Res. 2016 Mar;40(3):563-71. doi: 10.1111/acer.12972. Epub 2016 Feb 9. PubMed PMID: 26857541; PubMed Central PMCID: PMC4775356.

2: Wallenius K, Kjellstedt A, Thalén P, Löfgren L, Oakes ND. 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. PPAR Res. 2013;2013:305347. doi: 10.1155/2013/305347. Epub 2013 Oct 27. PubMed PMID: 24285952; PubMed Central PMCID: PMC3826326.

3: Zhang BC, Li XK, Che WL, Li WM, Hou L, Wei YD, Xu YW. [Peroxisome proliferator-activated receptor α/γ agonist tesaglitazar stabilizes atherosclerotic plaque in diabetic low density lipoprotein receptor knockout mice]. Zhonghua Xin Xue Guan Bing Za Zhi. 2013 Feb;41(2):143-9. Chinese. PubMed PMID: 23710746.

4: Zhang BC, Li WM, Li XK, Zhu MY, Che WL, Xu YW. Tesaglitazar ameliorates non-alcoholic fatty liver disease and atherosclerosis development in diabetic low-density lipoprotein receptor-deficient mice. Exp Ther Med. 2012 Dec;4(6):987-992. Epub 2012 Sep 17. PubMed PMID: 23226761; PubMed Central PMCID: PMC3494130.

5: 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. Tesaglitazar, a dual PPAR-α/γ agonist, hamster carcinogenicity, investigative animal and clinical studies. Toxicol Pathol. 2012;40(1):18-32. doi: 10.1177/0192623311429972. Epub 2011 Nov 30. PubMed PMID: 22131108.

6: Hamrén B, Ohman KP, Svensson MK, Karlsson MO. Pharmacokinetic-pharmacodynamic assessment of the interrelationships between tesaglitazar exposure and renal function in patients with type 2 diabetes mellitus. J Clin Pharmacol. 2012 Sep;52(9):1317-27. doi: 10.1177/0091270011416937. Epub 2011 Nov 1. PubMed PMID: 22045829.

7: Glinghammar B, Berg AL, Bjurström S, Stockling K, Blomgren B, Westerberg R, Skånberg I, Hellmold H, Andersson U. Proliferative and molecular effects of the dual PPARalpha/gamma agonist tesaglitazar in rat adipose tissues: relevance for induction of fibrosarcoma. Toxicol Pathol. 2011 Feb;39(2):325-36. doi: 10.1177/0192623310394210. Epub 2011 Jan 26. PubMed PMID: 21270424.

8: Liao J, Soltani Z, Ebenezer P, Isidro-Carrión AA, Zhang R, Asghar A, Aguilar E, Francis J, Hu X, Ferder L, Reisin E. Tesaglitazar, a dual peroxisome proliferator-activated receptor agonist (PPAR alpha/gamma), improves metabolic abnormalities and reduces renal injury in obese Zucker rats. Nephron Exp Nephrol. 2010;114(2):e61-8. doi: 10.1159/000254567. Epub 2009 Nov 4. PubMed PMID: 19887847.

9: van der Hoorn JW, Jukema JW, Havekes LM, Lundholm E, Camejo G, Rensen PC, Princen HM. The dual PPARalpha/gamma agonist tesaglitazar blocks progression of pre-existing atherosclerosis in APOE*3Leiden.CETP transgenic mice. Br J Pharmacol. 2009 Apr;156(7):1067-75. doi: 10.1111/j.1476-5381.2008.00109.x. Epub 2009 Feb 13. PubMed PMID: 19220285; PubMed Central PMCID: PMC2697696.

10: Hamrén B, Björk E, Sunzel M, Karlsson M. Models for plasma glucose, HbA1c, and hemoglobin interrelationships in patients with type 2 diabetes following tesaglitazar treatment. Clin Pharmacol Ther. 2008 Aug;84(2):228-35. doi: 10.1038/clpt.2008.2. Epub 2008 Mar 19. PubMed PMID: 18388881.

11: Hamrén B, Ericsson H, Samuelsson O, Karlsson MO. Mechanistic modelling of tesaglitazar pharmacokinetic data in subjects with various degrees of renal function--evidence of interconversion. Br J Clin Pharmacol. 2008 Jun;65(6):855-63. doi: 10.1111/j.1365-2125.2008.03110.x. Epub 2008 Feb 21. PubMed PMID: 18294322; PubMed Central PMCID: PMC2485221.

12: Ratner RE, Parikh S, Tou C; GALLANT 9 Study Group. Efficacy, safety and tolerability of tesaglitazar when added to the therapeutic regimen of poorly controlled insulin-treated patients with type 2 diabetes. Diab Vasc Dis Res. 2007 Sep;4(3):214-21. PubMed PMID: 17907111.

13: Göke B, Gause-Nilsson I, Persson A; GALLANT 8 Study Group. The effects of tesaglitazar as add-on treatment to metformin in patients with poorly controlled type 2 diabetes. Diab Vasc Dis Res. 2007 Sep;4(3):204-13. PubMed PMID: 17907110.

14: Wilding JP, Gause-Nilsson I, Persson A; GALLANT 7 Study Group. Tesaglitazar, as add-on therapy to sulphonylurea, dose-dependently improves glucose and lipid abnormalities in patients with type 2 diabetes. Diab Vasc Dis Res. 2007 Sep;4(3):194-203. PubMed PMID: 17907109.

15: Bays H, McElhattan J, Bryzinski BS; GALLANT 6 Study Group. A double-blind, randomised trial of tesaglitazar versus pioglitazone in patients with type 2 diabetes mellitus. Diab Vasc Dis Res. 2007 Sep;4(3):181-93. PubMed PMID: 17907108.

16: Fagerberg B, Schuster H, Birketvedt GS, Tonstad S, Ohman KP, Gause-Nilsson I; SIR Study Group. Improvement of postprandial lipid handling and glucose tolerance in a non-diabetic population by the dual PPARalpha/gamma agonist, tesaglitazar. Diab Vasc Dis Res. 2007 Sep;4(3):174-80. PubMed PMID: 17907107.

17: Bailey CJ. Learning from tesaglitazar. Diab Vasc Dis Res. 2007 Sep;4(3):161-2. PubMed PMID: 17907105.

18: Tonstad S, Retterstøl K, Ose L, Ohman KP, Lindberg MB, Svensson M. The dual peroxisome proliferator-activated receptor alpha/gamma agonist tesaglitazar further improves the lipid profile in dyslipidemic subjects treated with atorvastatin. Metabolism. 2007 Sep;56(9):1285-92. PubMed PMID: 17697874.

19: Schuster H, Fagerberg B, Edwards S, Halmos T, Lopatynski J, Stender S, Birketvedt GS, Tonstad S, Gause-Nilsson I, Halldórsdóttir S, Ohman KP; SIR Investigators. Tesaglitazar, a dual peroxisome proliferator-activated receptor alpha/gamma agonist, improves apolipoprotein levels in non-diabetic subjects with insulin resistance. Atherosclerosis. 2008 Mar;197(1):355-62. Epub 2007 Jul 13. PubMed PMID: 17631296.

20: Cha DR, Zhang X, Zhang Y, Wu J, Su D, Han JY, Fang X, Yu B, Breyer MD, Guan Y. Peroxisome proliferator activated receptor alpha/gamma dual agonist tesaglitazar attenuates diabetic nephropathy in db/db mice. Diabetes. 2007 Aug;56(8):2036-45. Epub 2007 May 29. PubMed PMID: 17536062.