1. GPCR/G Protein Neuronal Signaling Anti-infection
  2. Adrenergic Receptor Bacterial
  3. Propranolol

Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

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Propranolol Chemical Structure

Propranolol Chemical Structure

CAS No. : 525-66-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 165 In-stock
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100 mg USD 150 In-stock
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Based on 23 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].

IC50 & Target

β adrenergic receptor

 

Cellular Effect
Cell Line Type Value Description References
A-375 IC50
59.5 μM
Compound: Propranolol
Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 32216987]
CHO IC50
> 300 μM
Compound: 14d
Cytotoxicity against CHO cells after 48 hrs by MTT assay
Cytotoxicity against CHO cells after 48 hrs by MTT assay
[PMID: 22196513]
HEK293 IC50
0.48 nM
Compound: Prop
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay
[PMID: 32686936]
HEK293 IC50
0.55 nM
Compound: Prop
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay
[PMID: 32686936]
HEK293 IC50
21 μM
Compound: Propranolol
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
2100 nM
Compound: Propranolol
Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
[PMID: 21300721]
HEK293 IC50
63.2 μM
Compound: propranolol
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HMEC-1 GI50
149 μM
Compound: Propranolol
Antiproliferative activity against human HMEC1 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis
Antiproliferative activity against human HMEC1 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis
[PMID: 23462711]
MDA-MB-231 GI50
205 μM
Compound: Propranolol
Antiproliferative activity against human MDA-MB-231 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis
Antiproliferative activity against human MDA-MB-231 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis
[PMID: 23462711]
MRC5 GI50
150 μM
Compound: Propranolol
Antiproliferative activity against human MRC5 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis
Antiproliferative activity against human MRC5 cells by measuring metabolic activity of cells after 72 hrs by spectrophotometric analysis
[PMID: 23462711]
SK-MEL-28 IC50
75.82 μM
Compound: Propranolol
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 32216987]
SK-MEL-5 IC50
62.21 μM
Compound: Propranolol
Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
[PMID: 32216987]
T98G IC50
75 μM
Compound: Rac-22
Antiproliferation activity against human T98G cells measured after 72 hrs by crystal violet staining based assay
Antiproliferation activity against human T98G cells measured after 72 hrs by crystal violet staining based assay
[PMID: 34115934]
Ventricular myocyte IC50
18 μM
Compound: Propranolol
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
18000 nM
Compound: Propranolol
Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
[PMID: 21300721]
In Vitro

Propranolol (10-7 M-10-3 M; 24 and 48 hours) increases the total ERK1/2 levels in a dose-dependent manner, and ERK1/2 activation is observed specifically at 10-5 M in HemSCs[4].
? Propranolol (10-9 M-10-3 M; 24 and 48 hours) significant decreases cell proliferation at 10-4 M propranolol after 24 hours and 10-9 M propranolol after 48 hours in HemSCs[4].
? Propranolol (50 μM-200 μM;24 hours) increases Annexin V positivity and caspase-3 activation, rapidly induces HemSC apoptosis[4].

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

Western Blot Analysis[4]

Cell Line: HemSC cells
Concentration: 10-7 M-10-3 M
Incubation Time: 24 and 48 hours
Result: Increased the total ERK1/2 levels in a dose-dependent manner.

Cell Proliferation Assay[4]

Cell Line: HemSC cells
Concentration: 10-9 M-10-3 M
Incubation Time: 24 and 48 hours
Result: Suppressed HemSC proliferation.

Apoptosis Analysis[4]

Cell Line: HemSC cells
Concentration: 50 μM, 100 μM, or 200 μM
Incubation Time: 24 hours
Result: Induced HemSC cell death occurred via an apoptotic pathway.
In Vivo

Propranolol (orally administration; 40 mg/kg; daily) significantly reduces the vessel diameter relative to the vehicle-treated implants, and increases the number of cells that expressed phosphorylated ERK1/2 within the IH Matrigel implant[4].

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

Animal Model: A xenograft mouse model of IH (infantile hemangiomas ) with HemSC cells[4]
Dosage: 40 mg/kg
Administration: Orally administration; 40 mg/kg; daily
Result: Improved vessel development in the IH mouse model that correlated with MAPK pathway activation.
Clinical Trial
Molecular Weight

259.34

Formula

C16H21NO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(COC1=C2C=CC=CC2=CC=C1)CNC(C)C

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (385.59 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 3.8559 mL 19.2797 mL 38.5594 mL
5 mM 0.7712 mL 3.8559 mL 7.7119 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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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: ≥ 2.5 mg/mL (9.64 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.64 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.
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.
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).
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.
Purity & Documentation

Purity: 99.87%

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8559 mL 19.2797 mL 38.5594 mL 96.3986 mL
5 mM 0.7712 mL 3.8559 mL 7.7119 mL 19.2797 mL
10 mM 0.3856 mL 1.9280 mL 3.8559 mL 9.6399 mL
15 mM 0.2571 mL 1.2853 mL 2.5706 mL 6.4266 mL
20 mM 0.1928 mL 0.9640 mL 1.9280 mL 4.8199 mL
25 mM 0.1542 mL 0.7712 mL 1.5424 mL 3.8559 mL
30 mM 0.1285 mL 0.6427 mL 1.2853 mL 3.2133 mL
40 mM 0.0964 mL 0.4820 mL 0.9640 mL 2.4100 mL
50 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.9280 mL
60 mM 0.0643 mL 0.3213 mL 0.6427 mL 1.6066 mL
80 mM 0.0482 mL 0.2410 mL 0.4820 mL 1.2050 mL
100 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.9640 mL
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  • 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.

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Propranolol
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HY-B0573B
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