Phentolamine hydrochloride

Name: Phentolamine hydrochloride
Brand: MedChemExpress
SKU: HY-12717A
Rating: 5.0 (6 reviews)

Art. -Nr.: HY-12717A Reinheit: 99.91%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Phentolamine hydrochloride is an orally active, selective α1 and α2 Adrenergic receptor antagonist. Phentolamine hydrochloride antagonizes the vasodilatory effect of Cromakalim (HY-110011) on isolated circumflex coronary artery segments in dogs. Phentolamine hydrochloride reduces systemic vascular resistance and increases cardiac output. Phentolamine hydrochloride improves erectile dysfunction. Phentolamine hydrochloride can be used for the research of erectile dysfunction.

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Phentolamine hydrochloride Chemische Struktur

CAS. Nr. : 73-05-2

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
200 mg	Angebot einholen
500 mg	Angebot einholen

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This product is a controlled substance and not for sale in your territory.

Kundenbewertung

Based on 6 publication(s) in Google Scholar

Other Forms of Phentolamine hydrochloride:

Phentolamine In-stock
Phentolamine mesylate In-stock
Phentolamine-d₄ hydrochloride Angebot einholen
Phentolamine hydrochloride (Standard) Angebot einholen

6 Publications Citing Use of MCE Phentolamine hydrochloride

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

α adrenergic receptor β adrenergic receptor

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

IC₅₀ & Target^[1]

α1-adrenergic receptor

α2-adrenergic receptor

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1.1 1 Compound: Phentolamine	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	[PMID: 26005522]
CHO	IC₅₀	10.8 1 Compound: Phentolamine	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	[PMID: 26005522]
CHO	IC₅₀	12.5 1 Compound: Phentolamine	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	[PMID: 26005522]

In Vitro

Phentolamine hydrochloride (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.

Molekulargewicht

317.82

Formel

C₁₇H₂₀ClN₃O

CAS. Nr.

73-05-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=CC=CC(N(CC2=NCCN2)C3=CC=C(C)C=C3)=C1.[H]Cl

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 116.67 mg/mL (367.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1464 mL	15.7322 mL	31.4643 mL
5 mM	0.6293 mL	3.1464 mL	6.2929 mL
10 mM	0.3146 mL	1.5732 mL	3.1464 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.

Molaritätsrechner
Verdünnungsrechner

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (6.54 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.08 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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 and light)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Reinheit & Dokumentation

Purity: 99.91%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (252 KB) HNMR (255 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

Verweise

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

[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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1464 mL	15.7322 mL	31.4644 mL	78.6609 mL
	5 mM	0.6293 mL	3.1464 mL	6.2929 mL	15.7322 mL
	10 mM	0.3146 mL	1.5732 mL	3.1464 mL	7.8661 mL
	15 mM	0.2098 mL	1.0488 mL	2.0976 mL	5.2441 mL
	20 mM	0.1573 mL	0.7866 mL	1.5732 mL	3.9330 mL
	25 mM	0.1259 mL	0.6293 mL	1.2586 mL	3.1464 mL
	30 mM	0.1049 mL	0.5244 mL	1.0488 mL	2.6220 mL
	40 mM	0.0787 mL	0.3933 mL	0.7866 mL	1.9665 mL
	50 mM	0.0629 mL	0.3146 mL	0.6293 mL	1.5732 mL
	60 mM	0.0524 mL	0.2622 mL	0.5244 mL	1.3110 mL
	80 mM	0.0393 mL	0.1967 mL	0.3933 mL	0.9833 mL
	100 mM	0.0315 mL	0.1573 mL	0.3146 mL	0.7866 mL