2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Phentolamine mesylate

Phentolamine mesylate  (Synonyms: Phentolamine methanesulfonate)

Cat. No.: HY-B0362A Purity: 99.87%
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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.

Phentolamine mesylate Chemical Structure

Phentolamine mesylate Chemical Structure

CAS No. : 65-28-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in Water USD 73 In-stock
Solid
100 mg USD 66 In-stock
500 mg USD 198 In-stock
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Based on 4 publication(s) in Google Scholar

Other Forms of Phentolamine mesylate:

Phentolamine mesylate Related Antibodies

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View All Adrenergic Receptor Isoform Specific Products:

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α adrenergic receptor β adrenergic receptor

  • Biological Activity

  • Purity & Documentation

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Description

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[1][2][3].

IC50 & Target

α adrenergic receptor

 

In Vitro

Phentolamine (0.1-1 μM) inhibits the response to Clonidine in rat ileum, with the pA2 and pKB 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.

Phentolamine mesylate Related Antibodies
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.
Clinical Trial
Molecular Weight

377.46

Formula

C18H23N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (132.46 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6493 mL 13.2464 mL 26.4929 mL
5 mM 0.5299 mL 2.6493 mL 5.2986 mL
View the 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 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.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: 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
References

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 and light). 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
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.

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Phentolamine mesylate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Phentolamine65-28-1Adrenergic ReceptorBeta Receptorα1α2adrenergicbloodvesselsperipheralvascularresistancepheochromocytomahypertensionheartfailureerectiledysfunctionInhibitorinhibitorinhibit

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