Palosuran
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MedKoo CAT#: 329464

CAS#: 540769-28-6

Description: Palosuran, also known as ACT-058362, is a Urotensin-II receptor antagonist. Urotensin inhibition with palosuran could be a promising alternative in pulmonary arterial hypertension. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Palosuran improves pancreatic and renal function in diabetic rats.


Price and Availability

Size
Price

100mg
USD 950
1g
USD 3650
Size
Price

200mg
USD 1650
2g
USD 4850
Size
Price

500mg
USD 2450
5g
USD 7450

Palosuran, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 329464
Name: Palosuran
CAS#: 540769-28-6
Chemical Formula: C25H30N4O2
Exact Mass: 418.2369
Molecular Weight: 418.541
Elemental Analysis: C, 71.74; H, 7.23; N, 13.39; O, 7.65


Synonym: Palosuran; ACT-058362; ACT058362; ACT 058362.

IUPAC/Chemical Name: 1-(2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl)-3-(2-methylquinolin-4-yl)urea

InChi Key: WYJCYXOCHXWTHG-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: O=C(NC1=CC(C)=NC2=CC=CC=C12)NCCN3CCC(CC4=CC=CC=C4)(O)CC3


Technical Data

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).

Harmonized System Code:
293490


References

1: Pehlivan Y, Dokuyucu R, Demir T, Kaplan DS, Koc I, Orkmez M, Turkbeyler IH, Ceribasi AO, Tutar E, Taysi S, Kisacik B, Onat AM. Palosuran treatment effective as bosentan in the treatment model of pulmonary arterial hypertension. Inflammation. 2014 Aug;37(4):1280-8. doi: 10.1007/s10753-014-9855-8. PubMed PMID: 24604341.

2: Onat AM, Pehlivan Y, Turkbeyler IH, Demir T, Kaplan DS, Ceribasi AO, Orkmez M, Tutar E, Taysi S, Sayarlioglu M, Kisacik B. Urotensin inhibition with palosuran could be a promising alternative in pulmonary arterial hypertension. Inflammation. 2013 Apr;36(2):405-12. doi: 10.1007/s10753-012-9559-x. PubMed PMID: 23100033.

3: Demir T, Turkbeyler I, Kaplan DS, Pehlivan Y, Orkmez M, Tutar E, Taysi S, Kisacik B, Onat AM, Bagcı C. Effectiveness of palosuran in bleomycin-induced experimental scleroderma. Inflammation. 2013 Feb;36(1):75-9. doi: 10.1007/s10753-012-9521-y. PubMed PMID: 22886350.

4: 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.. Effect of the urotensin receptor antagonist palosuran in hypertensive patients with type 2 diabetic nephropathy. Hypertension. 2010 May;55(5):1206-9. doi: 10.1161/HYPERTENSIONAHA.109.149559. PubMed PMID: 20231521.

5: Sidharta PN, Rave K, Heinemann L, Chiossi E, Krähenbühl S, Dingemanse J. Effect of the urotensin-II receptor antagonist palosuran on secretion of and sensitivity to insulin in patients with Type 2 diabetes mellitus. Br J Clin Pharmacol. 2009 Oct;68(4):502-10. doi: 10.1111/j.1365-2125.2009.03480.x. PubMed PMID: 19843053; PubMed Central PMCID: PMC2780275.

6: Sidharta PN, van Giersbergen PL, Dingemanse J. Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects. J Clin Pharmacol. 2009 Oct;49(10):1168-75. doi: 10.1177/0091270009341181. PubMed PMID: 19625629.

7: 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. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br J Pharmacol. 2008 Oct;155(3):374-86. doi: 10.1038/bjp.2008.266. PubMed PMID: 18587423; PubMed Central PMCID: PMC2567886.

8: Trebicka J, Leifeld L, Hennenberg M, Biecker E, Eckhardt A, Fischer N, Pröbsting AS, Clemens C, Lammert F, Sauerbruch T, Heller J. Hemodynamic effects of urotensin II and its specific receptor antagonist palosuran in cirrhotic rats. Hepatology. 2008 Apr;47(4):1264-76. doi: 10.1002/hep.22170. PubMed PMID: 18318439.

9: Sidharta PN, Wagner FD, Bohnemeier H, Jungnik A, Halabi A, Krähenbühl S, Chadha-Boreham H, Dingemanse J. Pharmacodynamics and pharmacokinetics of the urotensin II receptor antagonist palosuran in macroalbuminuric, diabetic patients. Clin Pharmacol Ther. 2006 Sep;80(3):246-56. PubMed PMID: 16952491.

10: Clozel M, Hess P, Qiu C, Ding SS, Rey M. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21. PubMed PMID: 16267137.

11: Clozel M, Binkert C, Birker-Robaczewska M, Boukhadra C, Ding SS, Fischli W, Hess P, Mathys B, Morrison K, Müller C, Müller C, Nayler O, Qiu C, Rey M, Scherz MW, Velker J, Weller T, Xi JF, Ziltener P. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System. J Pharmacol Exp Ther. 2004 Oct;311(1):204-12. PubMed PMID: 15146030.