Palosuran hydrochloride
Based on 4 publication(s) in Google Scholar
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.
- Purity: 98.67%
- CAS No.: 2469274-58-4
- Formula: C25H31ClN4O2
- Molecular Weight:454.99
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Palosuran hydrochloride
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Biological Activity
IC50: 3.6 nM (human urotensin II receptor)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats with renal ischemia and reperfusion[1]
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Dosage:20 mg/kg/h for 135 min
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Administration:I.v. (continuous infusion) for 135 min
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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).
Chemical Information
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CAS No. 2469274-58-4
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Appearance Solid
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Molecular Weight 454.99
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Formula C25H31ClN4O2
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Color White to off-white
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SMILES
OC(CC1=CC=CC=C1)(CC2)CCN2CCNC(NC3=CC(C)=NC4=CC=CC=C34)=O.[H]Cl
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Synonyms
ACT-058362 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
The urotensin II receptor triggers an early meningeal response and a delayed macrophage-dependent vasospasm after subarachnoid hemorrhage in male mice. [Abstract]2024 Sep 29;15(1):8430. PMID: 39341842 -
Pharmacol Res
Urotensin receptor acts as a novel target for ameliorating fasting-induced skeletal muscle atrophy. [Abstract]2022 Nov:185:106468. PMID: 36167277 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Endocrinology
Inhibition of A-Type K+ Channels by Urotensin-II Induces Sensory Neuronal Hyperexcitability Through the PKCα-ERK Pathway. [Abstract]2018 May 1;159(5):2253-2263. PMID: 29648633
Solvent & Solubility
DMSO : 50 mg/mL (109.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 7.14 mg/mL (15.69 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1979 mL | 10.9893 mL | 21.9785 mL | 54.9463 mL |
| 5 mM | 0.4396 mL | 2.1979 mL | 4.3957 mL | 10.9893 mL | |
| 10 mM | 0.2198 mL | 1.0989 mL | 2.1979 mL | 5.4946 mL | |
| 15 mM | 0.1465 mL | 0.7326 mL | 1.4652 mL | 3.6631 mL | |
| DMSO | 20 mM | 0.1099 mL | 0.5495 mL | 1.0989 mL | 2.7473 mL |
| 25 mM | 0.0879 mL | 0.4396 mL | 0.8791 mL | 2.1979 mL | |
| 30 mM | 0.0733 mL | 0.3663 mL | 0.7326 mL | 1.8315 mL | |
| 40 mM | 0.0549 mL | 0.2747 mL | 0.5495 mL | 1.3737 mL | |
| 50 mM | 0.0440 mL | 0.2198 mL | 0.4396 mL | 1.0989 mL | |
| 60 mM | 0.0366 mL | 0.1832 mL | 0.3663 mL | 0.9158 mL | |
| 80 mM | 0.0275 mL | 0.1374 mL | 0.2747 mL | 0.6868 mL | |
| 100 mM | 0.0220 mL | 0.1099 mL | 0.2198 mL | 0.5495 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Palosuran hydrochloride Related Classifications
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