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Purity: ≥98%
Phenoxybenzamine HCl (formerly NSC-37448; NSC37448; Dibenzyline, NCI-C01661, NCIC01661; NCI-c01661), the hydrochloride salt of Phenoxybenzamine, is a potent, non-specific, irreversible alpha-adrenergic receptor antagonist with antihypertensive effects. Its IC50 of 550 nM indicates that it inhibits the alpha-adrenergic receptor. In particular, hypertension brought on by pheochromocytoma has been treated with phenoxybenzamine. When it comes to other a-blockers, its action starts later and lasts longer. Even though it is rarely used now, it was the first alpha blocker to be used for the treatment of benign prostatic hyperplasia.
| Targets |
α-adrenoceptor
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| Cell Assay |
Following cytometry, 1x3 cells are seeded in a 96-well plate with 100 μL of DMEM that has been enhanced with 10% FBS. WST-1 (Water Soluble Tetrazolium) is added to cells in ten microliters (10% of the total volume) and incubated for 30 min at 37°C before the colorimetric assay with 450 nm excitation and 630 nm emission at 24 h intervals up to 96 h. The standard curve is used to calculate the cell number after the mean fluorescence value has been counted.
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| Additional Infomation |
Phenoxybenzamine Hydrochloride can cause cancer according to an independent committee of scientific and health experts.
Phenoxybenzamine hydrochloride is a white crystalline powder. Melting point 137.5-140 °C. Used as an antihypertensive drug. Phenoxybenzamine hydrochloride is an organic molecular entity. Phenoxybenzamine Hydrochloride is the hydrochloride salt form of phenoxybenzamine, a synthetic, dibenzamine alpha-adrenergic antagonist with antihypertensive and vasodilatory properties. Phenoxybenzamine non-selectively and irreversibly blocks the postsynaptic alpha-adrenergic receptor in smooth muscle, thereby preventing vasoconstriction, relieving vasospasms, and decreasing peripheral resistance. Reflex tachycardia may occur and may be enhanced by blockade of alpha-2 receptors which enhances norepinephrine release. Phenoxybenzamine is reasonably anticipated to be a human carcinogen. An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. See also: Phenoxybenzamine (has active moiety). |
| Molecular Formula |
C18H23CL2NO
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| Molecular Weight |
340.3
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| Exact Mass |
339.115
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| Elemental Analysis |
C, 63.53; H, 6.81; Cl, 20.84; N, 4.12; O, 4.70
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| CAS # |
63-92-3
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| Related CAS # |
Phenoxybenzamine; 59-96-1; Phenoxybenzamine-d5 hydrochloride; 1329838-45-0; Phenoxybenzamine (benzyl-2,3,4,5,6-d5) (hydrochloride); 1398065-71-8
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| PubChem CID |
5284441
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| Appearance |
White to off-white crystalline powder
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| Boiling Point |
381.5ºC at 760 mmHg
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| Melting Point |
137.5°C
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| Flash Point |
184.5ºC
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| LogP |
4.996
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
22
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| Complexity |
262
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC([H])([H])C([H])([H])N(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])(C([H])([H])[H])C([H])([H])OC1C([H])=C([H])C([H])=C([H])C=1[H].Cl[H]
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| InChi Key |
VBCPVIWPDJVHAN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22ClNO.ClH/c1-16(15-21-18-10-6-3-7-11-18)20(13-12-19)14-17-8-4-2-5-9-17;/h2-11,16H,12-15H2,1H3;1H
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| Chemical Name |
N-benzyl-N-(2-chloroethyl)-1-phenoxypropan-2-amine;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9386 mL | 14.6929 mL | 29.3858 mL | |
| 5 mM | 0.5877 mL | 2.9386 mL | 5.8772 mL | |
| 10 mM | 0.2939 mL | 1.4693 mL | 2.9386 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05702944 | Recruiting | Drug: Phenoxybenzamine | Pheochromocytoma Paraganglioma |
Seoul National University Hospital |
January 18, 2023 | Phase 4 |
| NCT01379898 | Completed | Drug: Phenoxybenzamine Drug: Doxazosin |
Pheochromocytoma | University Medical Center Groningen |
December 2011 | Phase 4 |
| NCT00569855 | Completed | Drug: Phenoxybenzamine | Open-heart Surgery Cardiopulmonary Bypass |
University of Arkansas | February 2001 | Phase 2 |
| NCT03176693 | Completed | Drug: Phenoxybenzamine Drug: Doxazosin |
Pheochromocytoma Paraganglioma |
University of California, Los Angeles |
May 5, 2017 | Phase 3 |
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