Urapidil hydrochloride
Based on 1 Customer Validation
Urapidil hydrochloride is an orally active and blood-brain barrier permeability α1-adrenoceptor antagonist and 5-HT1A receptor agonist with a pIC50 of 6.13 and 4.38 against α1- and α2-adrenoceptor, respectively. Urapidil hydrochloride shows antihypertensive effect.
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- Pureza : 99.86%
- No. CAS: 64887-14-5
- Fòrmula: C20H30ClN5O3
- Peso molecular:423.94
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas 5-HT Receptor
MoreVer todos los productos específicos de isoformas Adrenergic Receptor
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Actividad biológica
Descripciòn
IC50 & Target
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5-HT1A Receptor |
α adrenergic receptor |
α1-adrenergic receptor 6.13 (pIC50) |
α2-adrenergic receptor 4.38 (pIC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 64887-14-5
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Appearance Solid
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Peso molecular 423.94
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Fòrmula C20H30ClN5O3
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Color White to off-white
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SMILES
O=C1N(C(C=C(N1C)NCCCN2CCN(CC2)C3=CC=CC=C3OC)=O)C.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
H2O : 100 mg/mL (235.88 mM; Need ultrasonic)
DMSO : 14.29 mg/mL (33.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
In Vivo:
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: ≥ 1.25 mg/mL (2.95 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.95 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (117.94 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocolo
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gross, G., G. Hanft, and N. Kolassa, Urapidil and some analogues with hypotensive properties show high affinities for 5-hydroxytryptamine (5-HT) binding sites of the 5-HT1A subtype and for alpha 1-adrenoceptor binding sites. Naunyn Schmiedebergs Arch Pharmacol, 1987. 336(6): p. 597-601. [Content Brief]
[2]. Buch, J., Urapidil, a dual-acting antihypertensive agent: Current usage considerations. Adv Ther, 2010. 27(7): p. 426-43. [Content Brief]
[3]. Vanhaesebrouck S, et al. Neonatal transient respiratory depression after maternal urapidil infusion for hypertension. Eur J Pediatr. 2009 Feb;168(2):221-3. [Content Brief]
[4]. Castor G, et al. Urapidil permeates the intact blood-brain barrier. Intensive Care Med. 1994;20(4):278-81. [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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.3588 mL | 11.7941 mL | 23.5882 mL | 58.9706 mL |
| 5 mM | 0.4718 mL | 2.3588 mL | 4.7176 mL | 11.7941 mL | |
| 10 mM | 0.2359 mL | 1.1794 mL | 2.3588 mL | 5.8971 mL | |
| 15 mM | 0.1573 mL | 0.7863 mL | 1.5725 mL | 3.9314 mL | |
| 20 mM | 0.1179 mL | 0.5897 mL | 1.1794 mL | 2.9485 mL | |
| 25 mM | 0.0944 mL | 0.4718 mL | 0.9435 mL | 2.3588 mL | |
| 30 mM | 0.0786 mL | 0.3931 mL | 0.7863 mL | 1.9657 mL | |
| H2O | 40 mM | 0.0590 mL | 0.2949 mL | 0.5897 mL | 1.4743 mL |
| 50 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 1.1794 mL | |
| 60 mM | 0.0393 mL | 0.1966 mL | 0.3931 mL | 0.9828 mL | |
| 80 mM | 0.0295 mL | 0.1474 mL | 0.2949 mL | 0.7371 mL | |
| 100 mM | 0.0236 mL | 0.1179 mL | 0.2359 mL | 0.5897 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.
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