Cat. No.: HY-B0362A

Phentolamine mesylate

(Synonyms: Phentolamine methanesulfonate)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.

For research use only. We do not sell to patients.

Purity: 99.90%
CAS No.: 65-28-1
Formula: C₁₈H₂₃N₃O₄S
Molecular Weight:377.46

Storage:

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Phentolamine mesylate Chemical Structure

CAS No.: 65-28-1

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

α adrenergic receptor

All Adrenergic Receptor Isoforms :

In Vitro

Phentolamine (0.1-1 μM) inhibits the response to Clonidine in rat ileum, with the pA₂ and pK_B of 7.92 and 8.07, respectively^[3].
Phentolamine (10-70 μg/mL; 48 h) inhibits proliferation of HDMECs and HBMECs in a dose-dependent manner, with IC₅₀s of 50 μg/mL and 30 μg/mL without toxicity, respectively^[4].
Phentolamine (10-20 or 20-40 μg/mL; 12-48 h) signi cantly delays scratch wound closure of HBMECs and HDMECs in a dose-dependent manner^[4].
Phentolamine (30 or 50 μg/mL; 4-12 h) inhibits tube formation of HBMECs and HDMECs^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Phentolamine (1 mg/kg; i.v.) produces hypotension and tachycardia in rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 65-28-1
Appearance Solid
Molecular Weight 377.46
Formula C₁₈H₂₃N₃O₄S
Color White to off-white
SMILES

CS(O)(=O)=O.CC1=CC=C(N(C2=CC(O)=CC=C2)CC3=NCCN3)C=C1
Synonyms

Phentolamine methanesulfonate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Publications (8)

All WBCell Migration/Invasion AssayIn Vivo Efficacy StudyIHC

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Journal Impact Factor

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 mesylate 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 mesylate 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.
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
Comput Struct Biotechnol J

2025 Dec 31;31:192-201.
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 mesylate 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 mesylate 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 mesylate 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.
SSRN

2026 Apr 30.
bioRxiv

2023 Oct 13.

Solvent & Solubility

In Vitro:

H₂O : ≥ 50 mg/mL (132.46 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6493 mL

13.2464 mL

26.4929 mL

5 mM

0.5299 mL

2.6493 mL

5.2986 mL

10 mM

0.2649 mL

1.3246 mL

2.6493 mL

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 and light). 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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (264.93 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gould L, et, al. Phentolamine. Am Heart J. 1976 Sep;92(3):397-402. [Content Brief]

[2]. Goldstein I, et, al. Oral phentolamine: an alpha-1, alpha-2 adrenergic antagonist for the treatment of erectile dysfunction. Int J Impot Res. 2000 Mar;12 Suppl 1:S75-80. [Content Brief]

[3]. Liu L, et, al. Evidence for functional alpha 2D-adrenoceptors in the rat intestine. Br J Pharmacol. 1996 Mar;117(5):787-92. [Content Brief]

[4]. Pan L, et, al. Phentolamine inhibits angiogenesis in vitro: Suppression of proliferation migration and differentiation of human endothelial cells. Clin Hemorheol Microcirc. 2017;65(1):31-41. [Content Brief]

[5]. Fioretti AC, et, al. Renal and femoral venous blood flows are regulated by different mechanisms dependent on α-adrenergic receptor subtypes and nitric oxide in anesthetized rats. Vascul Pharmacol. 2017 Dec;99:53-64. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	2.6493 mL	13.2464 mL	26.4929 mL	66.2322 mL
	5 mM	0.5299 mL	2.6493 mL	5.2986 mL	13.2464 mL
	10 mM	0.2649 mL	1.3246 mL	2.6493 mL	6.6232 mL
	15 mM	0.1766 mL	0.8831 mL	1.7662 mL	4.4155 mL
	20 mM	0.1325 mL	0.6623 mL	1.3246 mL	3.3116 mL
	25 mM	0.1060 mL	0.5299 mL	1.0597 mL	2.6493 mL
	30 mM	0.0883 mL	0.4415 mL	0.8831 mL	2.2077 mL
	40 mM	0.0662 mL	0.3312 mL	0.6623 mL	1.6558 mL
	50 mM	0.0530 mL	0.2649 mL	0.5299 mL	1.3246 mL
	60 mM	0.0442 mL	0.2208 mL	0.4415 mL	1.1039 mL
	80 mM	0.0331 mL	0.1656 mL	0.3312 mL	0.8279 mL
	100 mM	0.0265 mL	0.1325 mL	0.2649 mL	0.6623 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.

Phentolamine mesylate

8 Cited Publications

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Phentolamine mesylate

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Publications Citing Use of MedChemExpress (MCE) Phentolamine mesylate

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Phentolamine mesylate Related Classifications

HY-B0362A Related Classifications