Palosuran

• CAT Number: I003982
• CAS Number: 540769-28-6
• Molecular Formula: C25H30N4O2
• Molecular Weight: 418.53
• Purity: ≥95%
• Target: Urotensin Receptor (GPR14)
• Solubility: DMSO: ≥ 30 mg/mL
• Storage: Store at -20°C
• IC50: 3.6±0.2 nM [1]
• InChI: InChI=1S/C25H30N4O2/c1-19-17-23(21-9-5-6-10-22(21)27-19)28-24(30)26-13-16-29-14-11-25(31,12-15-29)18-20-7-3-2-4-8-20/h2-10,17,31H,11-16,18H2,1H3,(H2,26,27,28,30)
• InChIKey: WYJCYXOCHXWTHG-UHFFFAOYSA-N
• SMILES: O=C(NC1=CC(C)=NC2=CC=CC=C12)NCCN3CCC(CC4=CC=CC=C4)(O)CC3

Palosuran (Cat.No:I003982) is a selective antagonist of the chemokine receptor CCR2. It has been investigated for its potential therapeutic applications in the treatment of various inflammatory diseases, including diabetic nephropathy and chronic kidney disease. Palosuran shows promise in reducing inflammation and improving renal function, but further clinical studies are needed to determine its efficacy and safety.

Reference

1:Palosuran treatment effective as bosentan in the treatment model of pulmonary arterial hypertension. Pehlivan Y, Dokuyucu R, Demir T, Kaplan DS, Koc I, Orkmez M, Turkbeyler IH, Ceribasi AO, Tutar E, Taysi S, Kisacik B, Onat AM.Inflammation. 2014 Aug;37(4):1280-8. doi: 10.1007/s10753-014-9855-8. PMID: 24604341 2:Urotensin inhibition with palosuran could be a promising alternative in pulmonary arterial hypertension. Onat AM, Pehlivan Y, Turkbeyler IH, Demir T, Kaplan DS, Ceribasi AO, Orkmez M, Tutar E, Taysi S, Sayarlioglu M, Kisacik B.Inflammation. 2013 Apr;36(2):405-12. doi: 10.1007/s10753-012-9559-x. PMID: 23100033 3:Effectiveness of palosuran in bleomycin-induced experimental scleroderma. Demir T, Turkbeyler I, Kaplan DS, Pehlivan Y, Orkmez M, Tutar E, Taysi S, Kisacik B, Onat AM, Bagcı C.Inflammation. 2013 Feb;36(1):75-9. doi: 10.1007/s10753-012-9521-y. PMID: 22886350 4:Effect of the urotensin receptor antagonist palosuran in hypertensive patients with type 2 diabetic nephropathy. Vogt L, Chiurchiu C, Chadha-Boreham H, Danaietash P, Dingemanse J, Hadjadj S, Krum H, Navis G, Neuhart E, Parvanova AI, Ruggenenti P, Woittiez AJ, Zimlichman R, Remuzzi G, de Zeeuw D; PROLONG (PROteinuria Lowering with urOteNsin receptor antaGonists) Study Group..Hypertension. 2010 May;55(5):1206-9. doi: 10.1161/HYPERTENSIONAHA.109.149559. Epub 2010 Mar 15. PMID: 20231521 Free Article5:Effect of the urotensin-II receptor antagonist palosuran on secretion of and sensitivity to insulin in patients with Type 2 diabetes mellitus. Sidharta PN, Rave K, Heinemann L, Chiossi E, Krähenbühl S, Dingemanse J.Br J Clin Pharmacol. 2009 Oct;68(4):502-10. doi: 10.1111/j.1365-2125.2009.03480.x. PMID: 19843053 Free PMC Article6:Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects. Sidharta PN, van Giersbergen PL, Dingemanse J.J Clin Pharmacol. 2009 Oct;49(10):1168-75. doi: 10.1177/0091270009341181. Epub 2009 Jul 22. PMID: 19625629 7:Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Behm DJ, McAtee JJ, Dodson JW, Neeb MJ, Fries HE, Evans CA, Hernandez RR, Hoffman KD, Harrison SM, Lai JM, Wu C, Aiyar NV, Ohlstein EH, Douglas SA.Br J Pharmacol. 2008 Oct;155(3):374-86. doi: 10.1038/bjp.2008.266. Epub 2008 Jun 30. PMID: 18587423 Free PMC Article8:Hemodynamic effects of urotensin II and its specific receptor antagonist palosuran in cirrhotic rats. Trebicka J, Leifeld L, Hennenberg M, Biecker E, Eckhardt A, Fischer N, Pröbsting AS, Clemens C, Lammert F, Sauerbruch T, Heller J.Hepatology. 2008 Apr;47(4):1264-76. doi: 10.1002/hep.22170. PMID: 18318439 9:Pharmacodynamics and pharmacokinetics of the urotensin II receptor antagonist palosuran in macroalbuminuric, diabetic patients. Sidharta PN, Wagner FD, Bohnemeier H, Jungnik A, Halabi A, Krähenbühl S, Chadha-Boreham H, Dingemanse J.Clin Pharmacol Ther. 2006 Sep;80(3):246-56. PMID: 16952491 10:The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. Clozel M, Hess P, Qiu C, Ding SS, Rey M.J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21. Epub 2005 Nov 2. PMID: 16267137 Free Article