Phenoxybenzamine hydrochloride
Based on 1 publication(s) in Google Scholar
Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity.
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- Pureté: 99.53%
- CAS No.: 63-92-3
- Formule: C18H23Cl2NO
- Masse moléculaire:340.29
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Stockage:
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
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Phenoxybenzamine hydrochloride
MoreVoir tous les produits spécifiques à Isoform Adrenergic Receptor
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Activité biologique
α-adrenoceptor[1]
Phenoxybenzamine hydrochloride (0-100 μM; 96 h) markedly inhibits U251 and U87MG cells proliferation[2].
Phenoxybenzamine hydrochloride (10 μM; 24 h or 72 h) inhibits migration and invasion of U251 and U87MG cells[2].
Phenoxybenzamine hydrochloride (10 μM; 12 h) activates LINGO-1 and inhibits the TrkB-Akt pathway[2].
Phenoxybenzamine (0.1 μM-1 mM; 0-16 h) prevents hippocampal cell death after oxygen glucose deprivation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U251 and U87MG cells
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Concentration:0.1, 1, 10, 50 and 100 μM
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Incubation Time:96 h
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Result:Cell proliferation was inhibited markedly, the inhibition rate being 26.5 % for U251 cells and 27.3 % for U87MG cells at 10 μM.
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Cell Line:U251 and U87MG cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Apparent inhibition on migration was observed, and the inhibition rate was 28.6 and 39.8 % for U251 and U87MG, respectively.
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Cell Line:U251 and U87MG cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Attenuated the invasion properties of both U251 and U87MG markedly, as represented by the number of invaded cells per field declining from 365/field to 132/field (36.2 %) for U251 and 444/field to 298/field (67.1 %) for U87MG.
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Cell Line:U251
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Concentration:10 μM
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Incubation Time:12 h
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Result:Decreased the protein level of TrkB, p-TrkB, and p-Akt, but Akt remained unchanged significantly.
Phenoxybenzamine (1.0 mg/kg; i.v.; daily for 30 days) is neuroprotective in a rat model of severe traumatic brain injury[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice, U87MG tumor model[2]
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Dosage:20 nM
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Administration:Subcutaneous injection, 2-day interval for 26 days
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Result:Reduced the tumor cells.
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Animal Model:Male Wistar rats (350–500 g), traumatic brain injury (TBI) model[3]
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Dosage:1.0 mg/kg
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Administration:Intravenous injection, daily for 30 days
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Result:Showed significant improvements in neurological severity score (NSS) and foot fault scoring on days 14, 21, and 30. Reduced cognitive impairment associated with severe TBI and reduced the expression of pro-inflammatory genes.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 63-92-3
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Appearance Solid
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Masse moléculaire 340.29
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Formule C18H23Cl2NO
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Color White to off-white
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SMILES
CC(COC1=CC=CC=C1)N(CCCl)CC2=CC=CC=C2.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Protein Cell
Identification of serotonin 2A receptor as a novel HCV entry factor by a chemical biology strategy. [Abstract]2019 Mar;10(3):178-195. PMID: 29542010
Solvant et solubilité
DMSO : 100 mg/mL (293.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
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 (7.35 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 (7.35 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.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Habbe N, et al. Urapidil in the preoperative treatment of pheochromocytomas: a safe and cost-effective method. World J Surg. 2013 May;37(5):1141-6. [Content Brief]
[2]. Lin XB, et al. Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells. Tumour Biol. 2016 Mar;37(3):2901-8. [Content Brief]
[3]. Rau TF, et al. Phenoxybenzamine is neuroprotective in a rat model of severe traumatic brain injury. Int J Mol Sci. 2014 Jan 20;15(1):1402-17. [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 | 1 mM | 2.9387 mL | 14.6933 mL | 29.3867 mL | 73.4667 mL |
| 5 mM | 0.5877 mL | 2.9387 mL | 5.8773 mL | 14.6933 mL | |
| 10 mM | 0.2939 mL | 1.4693 mL | 2.9387 mL | 7.3467 mL | |
| 15 mM | 0.1959 mL | 0.9796 mL | 1.9591 mL | 4.8978 mL | |
| 20 mM | 0.1469 mL | 0.7347 mL | 1.4693 mL | 3.6733 mL | |
| 25 mM | 0.1175 mL | 0.5877 mL | 1.1755 mL | 2.9387 mL | |
| 30 mM | 0.0980 mL | 0.4898 mL | 0.9796 mL | 2.4489 mL | |
| 40 mM | 0.0735 mL | 0.3673 mL | 0.7347 mL | 1.8367 mL | |
| 50 mM | 0.0588 mL | 0.2939 mL | 0.5877 mL | 1.4693 mL | |
| 60 mM | 0.0490 mL | 0.2449 mL | 0.4898 mL | 1.2244 mL | |
| 80 mM | 0.0367 mL | 0.1837 mL | 0.3673 mL | 0.9183 mL | |
| 100 mM | 0.0294 mL | 0.1469 mL | 0.2939 mL | 0.7347 mL |
Phenoxybenzamine hydrochloride Related Classifications
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