Art. -Nr.: HY-14773

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Mirabegron

(Synonyms: YM178)

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

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

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Reinheit: 99.81%
CAS. Nr.: 223673-61-8
Formel: C₂₁H₂₄N₄O₂S
Molecular Weight:396.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Mirabegron Chemical Structure

CAS. Nr.: 223673-61-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

β adrenergic receptor

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 223673-61-8
Appearance Solid
Molecular Weight 396.51
Formel C₂₁H₂₄N₄O₂S
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
Synonyms

YM178
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

All In Vivo Efficacy StudyFlow Cytometry

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Journal Impact Factor

Cell Metab

Human Brown Adipocyte Thermogenesis Is Driven by β2-AR Stimulation. [Abstract]

2020 Aug 4;32(2):287-300.e7. PMID: 32755608
Adv Sci (Weinh)

Effective Prevention and Treatment of Acute Leukemias in Mice by Activation of Thermogenic Adipose Tissues. [Abstract]

2024 Oct;11(38):e2402332. PMID: 39049685

Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]

Schematic diagram of experimental design for testing anti-leukemia effects of combination therapy of chemo drugs and Mirabegron (10 mg/kg per day, oral). After transplantation for 7 days, leukemia-bearing mice were treated with combination therapy for up to 14 days.

Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]

Flow cytometry analysis of GFP⁺ cells in BM, PB, spleen, and liver in vehicle- or chemo-treated MLL-NRIP3 leukemia-bearing mice under vehicle or Mirabegron (10 mg/kg per day, oral) treatment.

Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]

Quantification of infiltrated leukemia cells in BM, spleen and liver in vehicle- or chemo-treated MLL-NRIP3 leukemia-bearing mice under vehicle or Mirabegron (10 mg/kg per day, oral) treatment.

Mirabegron purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Oct;11(38):e2402332. [Abstract]

Overall survival of vehicle- or chemo-treated MLL-NRIP3 leukemia‐bearing mice under vehicle or Mirabegron (10 mg/kg per day, oral) treatment.
J Transl Med

ZSWIM4 inhibition improves chemosensitivity in epithelial ovarian cancer cells by suppressing intracellular glycine biosynthesis. [Abstract]

2024 Feb 21;22(1):192. PMID: 38383406
Cardiovasc Drugs Ther

Mirabegron Ameliorated Atherosclerosis of ApoE-/- Mice in Chronic Intermittent Hypoxia but Not in Normoxia. [Abstract]

2022 Oct;36(5):805-815. PMID: 34152510
Patent

WO2015199097A1.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5220 mL

12.6100 mL

25.2200 mL

5 mM

0.5044 mL

2.5220 mL

5.0440 mL

10 mM

0.2522 mL

1.2610 mL

2.5220 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.25 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Takasu T, et al. Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. J Pharmacol Exp Ther. 2007 May;321(2):642-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Mirabegron

5 Cited Publications

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Mirabegron

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Publications Citing Use of MedChemExpress (MCE) Mirabegron

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mirabegron Related Classifications

HY-14773 Related Classifications