For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.<br>IC50 Value: 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ)<br>Target: PPARα/γ<br>Aleglitazar (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.</p>
| Catalog Number | I003657 |
| CAS Number | 475479-34-6 |
| Synonyms | (2S)-2-methoxy-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl]propanoic acid |
| Molecular Formula | C24H23NO5S |
| Purity | ≥95% |
| Target | PPAR |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 2.8 nM(PPAR-α); 4.6 nM(PPAR-γ) |
| InChI | InChI=1S/C24H23NO5S/c1-15-19(25-23(30-15)16-6-4-3-5-7-16)10-12-29-20-9-8-17(14-21(28-2)24(26)27)22-18(20)11-13-31-22/h3-9,11,13,21H,10,12,14H2,1-2H3,(H,26,27)/t21-/m0/s1 |
| InChIKey | DAYKLWSKQJBGCS-NRFANRHFSA-N |
| SMILES | CC1=C(N=C(O1)C2=CC=CC=C2)CCOC3=C4C=CSC4=C(C=C3)C[C@@H](C(=O)O)OC |
| Reference | </br>1:Non-clinical safety evaluation and risk assessment to human of aleglitazar, a dual PPAR α/γ agonist, and its major human metabolite. Bopst M, Atzpodien EA.Regul Toxicol Pharmacol. 2017 Mar 6;86:107-116. doi: 10.1016/j.yrtph.2017.03.003. [Epub ahead of print] PMID: 28274810 </br>2:Aleglitazar, a dual peroxisome proliferator-activated receptor-α and -γ agonist, protects cardiomyocytes against the adverse effects of hyperglycaemia. Chen Y, Chen H, Birnbaum Y, Nanhwan MK, Bajaj M, Ye Y, Qian J.Diab Vasc Dis Res. 2017 Mar;14(2):152-162. doi: 10.1177/1479164116679081. Epub 2017 Jan 23. PMID: 28111985 Free PMC Article</br>3:Therapeutic potential of the dual peroxisome proliferator activated receptor (PPAR)α/γ agonist aleglitazar in attenuating TNF-α-mediated inflammation and insulin resistance in human adipocytes. Massaro M, Scoditti E, Pellegrino M, Carluccio MA, Calabriso N, Wabitsch M, Storelli C, Wright M, De Caterina R.Pharmacol Res. 2016 May;107:125-36. doi: 10.1016/j.phrs.2016.02.027. Epub 2016 Mar 11. PMID: 26976796 </br>4:Aleglitazar, a Balanced Dual PPARα and -γ Agonist, Protects the Heart Against Ischemia-Reperfusion Injury. Qian J, Chen H, Birnbaum Y, Nanhwan MK, Bajaj M, Ye Y.Cardiovasc Drugs Ther. 2016 Apr;30(2):129-41. doi: 10.1007/s10557-016-6650-9. PMID: 26861490 </br>5:Aleglitazar, a dual peroxisome proliferator-activated receptor-α/γ agonist, improves insulin sensitivity, glucose control and lipid levels in people with type 2 diabetes: findings from a randomized, double-blind trial. Stirban AO, Andjelkovic M, Heise T, Nosek L, Fischer A, Gastaldelli A, Herz M.Diabetes Obes Metab. 2016 Jul;18(7):711-5. doi: 10.1111/dom.12620. Epub 2016 Feb 1. PMID: 26663152 </br>6:Effects of the dual peroxisome proliferator-activated receptor activator aleglitazar in patients with Type 2 Diabetes mellitus or prediabetes. Erdmann E, Califf R, Gerstein HC, Malmberg K, Ruilope L, Schwartz GG, Wedel H, Volz D, Ditmarsch M, Svensson A, Bengus M.Am Heart J. 2015 Jul;170(1):117-22. doi: 10.1016/j.ahj.2015.03.021. Epub 2015 Apr 2. PMID: 26093872 </br>7:Efficacy, safety and tolerability of aleglitazar in patients with type 2 diabetes: pooled findings from three randomized phase III trials. Henry RR, Buse JB, Wu H, Durrwell L, Mingrino R, Jaekel K, El Azzouzi B, Andjelkovic M, Herz M.Diabetes Obes Metab. 2015 Jun;17(6):560-5. doi: 10.1111/dom.12455. Epub 2015 Apr 8. PMID: 25728612 </br>8:Effects of the dual peroxisome proliferator-activated receptor-α/γ agonist aleglitazar on renal function in patients with stage 3 chronic kidney disease and type 2 diabetes: a Phase IIb, randomized study. Ruilope L, Hanefeld M, Lincoff AM, Viberti G, Meyer-Reigner S, Mudie N, Wieczorek Kirk D, Malmberg K, Herz M.BMC Nephrol. 2014 Nov 18;15:180. doi: 10.1186/1471-2369-15-180. PMID: 25407798 Free PMC Article</br>9:Acute coronary syndromes: Aleglitazar trial findings reported. Mearns BM.Nat Rev Cardiol. 2014 Jun;11(6):311. doi: 10.1038/nrcardio.2014.53. Epub 2014 Apr 15. No abstract available. PMID: 24736759 </br>10:Effect of aleglitazar on cardiovascular outcomes after acute coronary syndrome in patients with type 2 diabetes mellitus: the AleCardio randomized clinical trial. Lincoff AM, Tardif JC, Schwartz GG, Nicholls SJ, Rydén L, Neal B, Malmberg K, Wedel H, Buse JB, Henry RR, Weichert A, Cannata R, Svensson A, Volz D, Grobbee DE; AleCardio Investigators..JAMA. 2014 Apr 16;311(15):1515-25. doi: 10.1001/jama.2014.3321. PMID: 24682069 |
