[CAS NO. 2469274-58-4] Palosuran hydrochloride
PRODUCTS SPECIFICATIONS [2469274-58-4]
DESCRIPTION [2469274-58-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 454.99 |
| Molecular Formula | C25H31ClN4O2 |
| SMILES | OC(CC1=CC=CC=C1)(CC2)CCN2CCNC(NC3=CC(C)=NC4=CC=CC=C34)=O.[H]Cl |
2 Publications Citing Use of MCE
Summary
Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor , with an IC 50 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
125
I-U-II binding to human UT receptor, with IC
50
s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells
[1]
.
Palosuran inhibits Ca
2+
mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC
50
s 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 IC
50
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). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL ( 109.89 mM ; Need ultrasonic)
H 2 O : 7.14 mg/mL ( 15.69 mM ; Need ultrasonic)
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 |
References
- [1] Clozel M, et, al. 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
- [2] Clozel M, et, al. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21.