Palosuran

SKU: orb1224746

Description

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.

Key Properties

• CAS Number: 540769-28-6
• MW: 418.5313
• Purity: >98% (HPLC)
• Formula: C₂₅H₃₀N₄O₂
• SMILES: O=C(NC1=CC(C)=NC2=CC=CC=C12)NCCN3CCC(CC4=CC=CC=C4)(O)CC3
• Target: Urotensin Receptor
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• 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. 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.
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• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ACT058362 | ACT 058362 | ACT-058362

Quick Database Links

Gene Symbol

Urotensin Receptor