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

Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

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Mirabegron Chemical Structure

Mirabegron Chemical Structure

CAS No. : 223673-61-8

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Based on 4 publication(s) in Google Scholar

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Description

Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

IC50 & Target

β adrenergic receptor

 

In Vitro

Mirabegron (YM178) increases cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR). EC50 value is 22.4 nM. EC50 values of Mirabegron for human β1- and β2-ARs are 10,000 nM or more, respectively. EC50 of Mirabegron in rat bladder strips precontracted with 10-6 M Carbachol (CCh) is 5.1 μM, whereas that in human bladder strips precontracted with 10-7 M CCh is 0.78 μM. Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human β3-ARs, with an EC50 value and I.A. of 22.4 nM and 0.8, respectively. Mirabegron has little agonistic effect on β1- and β2-ARs. Compared by EC50 value, Mirabegron is approximately one third as potent as isoproterenol. The maximal relaxant effects of Mirabegron are 94±1%, that of CCh, indicating that Mirabegron acts a full agonist in the rat bladder. The maximal relaxant effects of Mirabegron is 89.4±2.3%[1].

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

In Vivo

Mirabegron (YM178) produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. In contrast, Mirabegron does not decrease the amplitude of rhythmic bladder contraction at up to 3 mg/kg i.v.. On the contrary, Oxybutynin significantly increases the frequency of rhythmic bladder contraction and decreased its amplitude at doses of 0.272 mg/kg i.v. or more[1].

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

Clinical Trial
Molecular Weight

396.51

Formula

C21H24N4O2S

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=CC=C(CCNC[C@H](O)C2=CC=CC=C2)C=C1)CC3=CSC(N)=N3

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 100 mg/mL (252.20 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 2.5220 mL 12.6100 mL 25.2200 mL
5 mM 0.5044 mL 2.5220 mL 5.0440 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
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

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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: ≥ 2.08 mg/mL (5.25 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 (5.25 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 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: 99.89%

References
Cell Assay
[1]

CHO cells (105) are seeded in each well of a 24-well culture plate and subcultured. Three days later, the medium is exchanged with 250 μL/well Hanks' balanced salt solution containing 0.1 mM 3-isobutyl-1-methylxanthine, pH 7.4. The cells are incubated with each compound (isoproterenol, Mirabegron, BRL37344, and CL316,243 at final concentrations of 10-10 to 10-4 M) for 10 min at 37°C, after which incubation is stopped by the addition of 250 μL of 0.2 M HCl. cAMP concentration in the reaction mixture is measured by radioimmunoassay using an 125I-cAMP assay system using a gamma counter. Fifty microliters of reaction mixture is incubated with 50 μL of succinyl agent for 10 min at room temperature, after which the reaction is stopped by the addition of 400 μL of buffer solution. Fifty microliters of succinylated sample is incubated with 50 μL of 125I-cAMP and 50 μL of anti-cAMP antibody for 24 h at 4°C. At the end of the incubation period, 250 μL of charcoal suspension is added and centrifuged for 10 min at 2800g at 4°C. Two hundred and fifty microliters of supernatant is transferred into a tube and counted for 1 min using a gamma counter. The intrinsic activity (I.A.) relative to isoproterenol for each β-adrenoceptor agonist is calculated using the maximal response of each compound[1].

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

Animal Administration
[1]

Rats[1]
Male (350 to 400 g) and female (225 to 290 g) Wistar rats are used. The free-form doses of 0.03, 0.1, 0.3, 1 and 3 mg/kg for Mirabegron and 0.0272, 0.0907, 0.272, 0.907, and 2.72 mg/kg for oxybutynin are used in this study.

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5220 mL 12.6100 mL 25.2200 mL 63.0501 mL
5 mM 0.5044 mL 2.5220 mL 5.0440 mL 12.6100 mL
10 mM 0.2522 mL 1.2610 mL 2.5220 mL 6.3050 mL
15 mM 0.1681 mL 0.8407 mL 1.6813 mL 4.2033 mL
20 mM 0.1261 mL 0.6305 mL 1.2610 mL 3.1525 mL
25 mM 0.1009 mL 0.5044 mL 1.0088 mL 2.5220 mL
30 mM 0.0841 mL 0.4203 mL 0.8407 mL 2.1017 mL
40 mM 0.0631 mL 0.3153 mL 0.6305 mL 1.5763 mL
50 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2610 mL
60 mM 0.0420 mL 0.2102 mL 0.4203 mL 1.0508 mL
80 mM 0.0315 mL 0.1576 mL 0.3153 mL 0.7881 mL
100 mM 0.0252 mL 0.1261 mL 0.2522 mL 0.6305 mL
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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.

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