Palosuran

Research use only, not for human use.

A potent and specific antagonist of human Urotensin (UT) receptor.

A potent and specific antagonist of human Urotensin (UT) receptor; inhibits 125I-U-II binding to human UT receptors in membrane preparations from CHO cells carrying the human UT receptors with IC50 of 3.6 nM; prevents the development of acute renal failure and the histological consequences of ischemia in rats.Ischemia Discontinued(In Vitro):Palosuran (8 h) inhibits 125I-U-II binding to human UT receptor, with IC50s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells.Palosuran inhibits Ca2+ mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC50s of 17 and >10000 nM, respectively.Palosuran (0.12-10000 nM; 20 min) inhibits human U-II induced MAPK phosphorylation in a dose-dependent manner in recombinant CHO cells, with an IC50 of 150 nM.(In Vivo):ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure.Palosuran (300 mg/kg/d; p.o. for 16 weeks) improves the survival, increases insulin, and slows the increase in glycemia, glycosylated hemoglobin, and serum lipids in streptozotocin-induced diabetic rats.

Palosuran (8 h) inhibits 125I-U-II binding to human UT receptor, with IC50s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells.Palosuran inhibits Ca2+ mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC50s of 17 and >10000 nM, respectively.Palosuran (0.12-10000 nM; 20 min) inhibits human U-II induced MAPK phosphorylation in a dose-dependent manner in recombinant CHO cells, with an IC50 of 150 nM.

ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure.Palosuran (300 mg/kg/d; p.o. for 16 weeks) improves the survival, increases insulin, and slows the increase in glycemia, glycosylated hemoglobin, and serum lipids in streptozotocin-induced diabetic rats. Animal Model:Male Wistar rats with renal ischemia and reperfusion Dosage:20 mg/kg/h for 135 min Administration:I.v. (continuous infusion) for 135 min Result:Restored renal blood flow to baseline values at 30 min after reperfusion and by 60 min increased renal blood flow by 12% above baseline values.

ACT058362 | ACT 058362 | ACT-058362

GPCR/G Protein

Urotensin Receptor

UrotensinReceptor(GPR14)

Cardiovascular Disease

Ischemia

540769-28-6

418.5313

C25H30N4O2

>98% (HPLC)

DMSO: ≥ 30 mg/mL

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

Urea, N-[2-[4-hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-methyl-4-quinolinyl)-

(-20℃)

With Ice Pack

≥ 2 years