1. GPCR/G Protein
  2. Urotensin Receptor
  3. Palosuran hydrochloride

Palosuran hydrochloride (Synonyms: ACT-058362 hydrochloride)

Cat. No.: HY-10655A Purity: 98.67%
Handling Instructions

Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats.

For research use only. We do not sell to patients.

Palosuran hydrochloride Chemical Structure

Palosuran hydrochloride Chemical Structure

CAS No. : 2469274-58-4

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10 mM * 1 mL USD 290 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats[1][2].

IC50 & Target

IC50: 3.6 nM (human urotensin II receptor)[1]

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[1].
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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats with renal ischemia and reperfusion[1]
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.
Did not significantly alter mean arterial blood pressure (MAP) and heart rate (HR).
Molecular Weight

454.99

Formula

C₂₅H₃₁ClN₄O₂

CAS No.

2469274-58-4

SMILES

OC(CC1=CC=CC=C1)(CC2)CCN2CCNC(NC3=CC(C)=NC4=CC=CC=C34)=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (10.99 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1979 mL 10.9893 mL 21.9785 mL
5 mM 0.4396 mL 2.1979 mL 4.3957 mL
10 mM 0.2198 mL 1.0989 mL 2.1979 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

PalosuranACT-058362ACT058362ACT 058362Urotensin ReceptorUT receptorurotensinIIpancreaticrenaldiabeticischemiareperfusionInhibitorinhibitorinhibit

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Product Name:
Palosuran hydrochloride
Cat. No.:
HY-10655A
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