1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Atenolol

Atenolol  (Synonyms: (RS)-Atenolol)

Cat. No.: HY-17498 Purity: 99.82%
COA Handling Instructions

Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.

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

Atenolol Chemical Structure

Atenolol Chemical Structure

CAS No. : 29122-68-7

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10 mM * 1 mL in DMSO
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Based on 12 publication(s) in Google Scholar

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Description

Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM at β1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris[1][2].

IC50 & Target[1]

Beta-1 adrenergic receptor

697 nM (Ki)

In Vitro

Atenolol (1-100 μM, 5 h) strengthenes the inhibitory effect on cell migration of rat aortic smooth muscle cells when combinated with Nifedipine (HY-B0284) (1-100μM)[3].
Atenolol (50-150 μM, 24 h) decreases the cell surival of Hem-ECs in a dose-dependent manner[4].

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

Cell Proliferation Assay[3]

Cell Line: Rat aortic smooth muscle cells
Concentration: 1-100 μM
Incubation Time: 48-72 h
Result: Inhibited cell proliferation (-20%) when incubation lasted 72 h at 100 μM.

Cell Migration Assay [3]

Cell Line: Rat aortic smooth muscle cells
Concentration: 1-100 μM
Incubation Time: 5 h
Result: Inhibited myocyte migration induced by fibrinogen in a dose-dependent manner.

Western Blot Analysis[4]

Cell Line: Hemangioma-derived ECs (Hem-ECs)
Concentration: 100 μM
Incubation Time: 6 h
Result: Increased LC3-Ⅱ/LC3-Ⅰ ratio and decreased p62.
In Vivo

Atenolol (5-20 mg/kg, i.g., one time) combinated with Amlodipine (HY-B0317) can reduce and stabilize blood oressure (BP) in 2K1C renovascular hypertensive rats[5].
Atenolol (6 mg/kg, p.o., one time) combinated with Nifedipine (HY-B0284) prevents ZD6126-induced cardiac necrosis and increases plasma troponin T levels[6].
Atenolol (40 mg/kg, p.o., daily, 6 weeks) increased plasma membrane β1- and β2- adrenoceptors density in rats[7].

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

Animal Model: 2K1C renovascular hypertensive rats [5]
Dosage: 5-20 mg/kg (single; combination with Amlodipine (HY-B0317) (0.5-2 mg/kg))
Administration: i.g., one time
Result: Reduced the average blood oressure (BP) levels within 24 h after administration when treated with Atenolol and Amlodipine (HY-B0317).
Decreased the blood pressure variability (BPV) levels when treated with 10 mg/kg Atenolol and 1 mg/kg Amlodipine (HY-B0317), or 20 mg/kg Atenolol and 2 mg/kg Amlodipine (HY-B0317).
Animal Model: Hras5 tumor xenograft rat model [6]
Dosage: 6 mg/kg (combination with Nifedipine (HY-B0284) (10 mg/kg))
Administration: Oral gavage (p.o.), one time
Result: Abolished the hypertensive and tachycaidic effects of ZD6126.
Animal Model: Male wistar rats[7]
Dosage: 40 mg/kg
Administration: Oral gavage (p.o.), daily, 6 weeks
Result: Increased the density of total β-adrenoceptors.
Decreased the expression level of β1- adrenoceptor mRNA.
Clinical Trial
Molecular Weight

266.34

Formula

C14H22N2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)CC1=CC=C(OCC(O)CNC(C)C)C=C1

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 (375.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 8.33 mg/mL (31.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7546 mL 18.7730 mL 37.5460 mL
5 mM 0.7509 mL 3.7546 mL 7.5092 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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

* 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

  • 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)

V1

=
Concentration (final)

C2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.39 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 (9.39 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.

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: 36.67 mg/mL (137.68 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.
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
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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.7546 mL 18.7730 mL 37.5460 mL 93.8650 mL
5 mM 0.7509 mL 3.7546 mL 7.5092 mL 18.7730 mL
10 mM 0.3755 mL 1.8773 mL 3.7546 mL 9.3865 mL
15 mM 0.2503 mL 1.2515 mL 2.5031 mL 6.2577 mL
20 mM 0.1877 mL 0.9386 mL 1.8773 mL 4.6932 mL
25 mM 0.1502 mL 0.7509 mL 1.5018 mL 3.7546 mL
30 mM 0.1252 mL 0.6258 mL 1.2515 mL 3.1288 mL
DMSO 40 mM 0.0939 mL 0.4693 mL 0.9386 mL 2.3466 mL
50 mM 0.0751 mL 0.3755 mL 0.7509 mL 1.8773 mL
60 mM 0.0626 mL 0.3129 mL 0.6258 mL 1.5644 mL
80 mM 0.0469 mL 0.2347 mL 0.4693 mL 1.1733 mL
100 mM 0.0375 mL 0.1877 mL 0.3755 mL 0.9386 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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  • 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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