Phentolamine
Based on 8 publication(s) in Google Scholar
Phentolamine is an orally active, selective α1 and α2 Adrenergic receptor antagonist. Phentolamine antagonizes the vasodilatory effect of Cromakalim (HY-110011) on isolated circumflex coronary artery segments in dogs. Phentolamine reduces systemic vascular resistance and increases cardiac output. Phentolamine improves erectile dysfunction. Phentolamine can be used for the research of erectile dysfunction.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 50-60-2
- Formula: C17H19N3O
- Molecular Weight:281.35
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Phentolamine
More- Acta Pharmacol Sin. 2026 May 29. [Abstract]
- Neurosci Bull. 2023 Dec;39(12):1789-1806. [Abstract]
- Comput Struct Biotechnol J. 2025 Dec 31;31:192-201.
- J Endocrinol. 2020 Mar;244(3):459-471. [Abstract]
- Insect Biochem Mol Biol. 2025 May:180:104312. [Abstract]
- J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
- SSRN. 2026 Apr 30.
- bioRxiv. 2023 Oct 13.
Customer Validation & Images
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Cell Migration/Invasion Assay
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Cell Migration/Invasion Assay
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IHC
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WB
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In Vivo Efficacy Study
All Adrenergic Receptor Isoforms
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Biological Activity
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α1-adrenergic receptor |
α2-adrenergic receptor |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
1.1 nM
Compound: Phentolamine
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Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
Displacement of [3H]-Prazosin from human alpha-1A adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
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[PMID: 26005522] |
| CHO | IC50 |
10.8 nM
Compound: Phentolamine
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Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
Displacement of [3H]-Prazosin from human alpha-1B adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
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[PMID: 26005522] |
| CHO | IC50 |
12.5 nM
Compound: Phentolamine
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Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
Displacement of [3H]-Prazosin from human alpha-1D adrenergic receptor transfected in CHO cell membranes after 2 hrs by microplate scintillation counting analysis
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[PMID: 26005522] |
Phentolamine (1-100 μM) concentration-dependently antagonizes the vasodilatory effect of Cromakalim on isolated circumflex coronary artery segments of dogs; at a concentration of 100 μM, it reduces the pD2 value of Cromakalim from 6.62 to 5.08[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:WT mice[3]
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Dosage:1 mg/kg
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Administration:IP
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Result:Reduced blood glucose and increased insulin levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 50-60-2
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Appearance Solid
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Molecular Weight 281.35
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Formula C17H19N3O
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Color White to off-white
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SMILES
OC1=CC=CC(N(CC2=NCCN2)C3=CC=C(C)C=C3)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Activation of peripheral muscarinic receptors rescues depressive-like behaviors via gut-brain-axis, involving parasympathetic excitation. [Abstract]2026 May 29. PMID: 42215618 -
Neurosci Bull
Peripheral BDNF Regulates Somatosensory-Sympathetic Coupling in Brachial Plexus Avulsion-Induced Neuropathic Pain. [Abstract]2023 Dec;39(12):1789-1806. PMID: 37335428
Phentolamine purchased from MedChemExpress. Usage Cited in: Neurosci Bull. 2023 Dec;39(12):1789-1806. [Abstract]
Phentolamine (0.5, 1 mg/kg; IP; once a day for 5 consecutive days) decreased the expression of BDNF, TrκB, and α2-AR after BPA.
Phentolamine purchased from MedChemExpress. Usage Cited in: Neurosci Bull. 2023 Dec;39(12):1789-1806. [Abstract]
Phentolamine (0.5, 1 mg/kg; IP; once a day for 5 consecutive days) increased the mechanical allodynia threshold of the affected ipsilateral forepaw and relieved the hypothermia in the ipsilateral forepaw and the edema in the ipsilateral forepaw of mice after BPA.
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J Endocrinol
miR-7 mediates the signaling pathway of NE affecting FSH and LH synthesis in pig pituitary. [Abstract]2020 Mar;244(3):459-471. PMID: 31905166 -
Insect Biochem Mol Biol
Molecular and pharmacological characterization of the dopamine receptors in the oriental fruit fly, Bactrocera dorsalis. [Abstract]2025 May:180:104312. PMID: 40245998 -
J Cancer
Pan-cancer analysis of the role of α2C-adrenergic receptor (ADRA2C) in human tumors and validation in glioblastoma multiforme models. [Abstract]2024 Sep 9;15(17):5691-5709. PMID: 39308687
Phentolamine purchased from MedChemExpress. Usage Cited in: J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
Phentolamine (10 μM; 24, 48 h) increased the migration speed in GL261 cells.
Phentolamine purchased from MedChemExpress. Usage Cited in: J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
Phentolamine (0.005 μM; 12, 24 h) increased the migration speed in U87 cells.
Phentolamine purchased from MedChemExpress. Usage Cited in: J Cancer. 2024 Sep 9;15(17):5691-5709. [Abstract]
Phentolamine (1 mg/kg; IP; every other day for 14 days) elevated the Bcl2/Bax ratio and MMP2 expression level in tumor tissues of mouse glioma models.
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Solvent & Solubility
DMSO : 116.67 mg/mL (414.68 mM; Need ultrasonic; 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. 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. 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 (8.89 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 (8.89 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.
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 (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Goldstein I I. Oral phentolamine: an alpha-1, alpha-2 adrenergic antagonist for the treatment of erectile dysfunction. Int J Impot Res. 2000 Mar;12(S1):S75-S80 [Content Brief]
[2]. Majid PA, et al. Phentolamine for vasodilator treatment of severe heart-failure. Lancet. 1971 Oct 2;2(7727):719-24. [Content Brief] [Content Brief]
[3]. McPherson GA, et al. Phentolamine and structurally related compounds selectively antagonize the vascular actions of the K+ channel opener, cromromakalim. Br J Pharmacol. 1989;97(3):941-949. [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. 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 |
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| DMSO | 1 mM | 3.5543 mL | 17.7715 mL | 35.5429 mL | 88.8573 mL |
| 5 mM | 0.7109 mL | 3.5543 mL | 7.1086 mL | 17.7715 mL | |
| 10 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL | 8.8857 mL | |
| 15 mM | 0.2370 mL | 1.1848 mL | 2.3695 mL | 5.9238 mL | |
| 20 mM | 0.1777 mL | 0.8886 mL | 1.7771 mL | 4.4429 mL | |
| 25 mM | 0.1422 mL | 0.7109 mL | 1.4217 mL | 3.5543 mL | |
| 30 mM | 0.1185 mL | 0.5924 mL | 1.1848 mL | 2.9619 mL | |
| 40 mM | 0.0889 mL | 0.4443 mL | 0.8886 mL | 2.2214 mL | |
| 50 mM | 0.0711 mL | 0.3554 mL | 0.7109 mL | 1.7771 mL | |
| 60 mM | 0.0592 mL | 0.2962 mL | 0.5924 mL | 1.4810 mL | |
| 80 mM | 0.0444 mL | 0.2221 mL | 0.4443 mL | 1.1107 mL | |
| 100 mM | 0.0355 mL | 0.1777 mL | 0.3554 mL | 0.8886 mL |
Phentolamine Related Classifications
HY-12717 Related Classifications
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