Mirabegron

Catalog No.S4009 Synonyms: YM 178

For research use only.

Mirabegron (YM 178) is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

Mirabegron Chemical Structure

CAS No. 223673-61-8

Selleck's Mirabegron has been cited by 10 Publications

Purity & Quality Control

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Biological Activity

Description Mirabegron (YM 178) is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
Targets
β3-adrenoceptor [1]
22.4 nM(EC50)
In vitro

Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human 3-adrenoceptors (ARs) with I.A. of 0.8. Mirabegron has little agonistic effect on 1- and 2-ARs. Mirabegron concentration-dependently relaxes rat and Human bladder smooth muscle strips precontracted with 10-6 M or 10-7 M carbachol with EC50 values of 5.1 μM and 0.78 μM, respectively. The maximal relaxant effects of Mirabegron are 94.0 % and 89.4% that of carbachol, respectively. [1] Mirabegron is a time-dependent inhibitor of CYP2D6 in the presence of NADPH as the IC50 value in human liver microsomes decreased from 13 to 4.3 μM after 30 min preincubation. Mirabegron acts partly as an irreversible or quasi-irreversible metabolism-dependent inhibitor of CYP2D6. [2]

In vivo Mirabegron produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. 3 mg/kg i.v. Mirabegron suppresses the frequency to 2 counts/10 min. Mirabegron does not decrease the amplitude of rhythmic bladder contraction. [1] Mirabegron decreases primary bladder afferent activity and bladder microcontractions in rats. Mirabegron (0.3 and 1 mg/kg) inhibits mechanosensitive single-unit afferent activities (SAAs) of Aδ fibers in response to bladder filling. SAAs of C-fibers decrease only at 1 mg/kg Mirabegron treatment. Mirabegron administration suppresses the mean bladder pressure and the number of microcontractions during an isovolumetric condition of the bladder. [3] Mirabegron is efficient on facilitation of bladder storage. Mirabegron dose-dependently decreases the resting intravesical pressure. Mirabegron dose dependently decreases the frequency of nonvoiding contractions, considered an index of abnormal response in bladder storage. Mirabegron exhibits no significant effects on the amplitude of nonvoiding contractions, micturition pressure, threshold pressure, voided volume, residual volume, or bladder capacity. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 79 mg/mL
(199.23 mM)
Ethanol 8 mg/mL
(20.17 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

11mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 396.51
Formula

C21H24N4O2S

CAS No. 223673-61-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)C(CNCCC2=CC=C(C=C2)NC(=O)CC3=CSC(=N3)N)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05040984 Recruiting Drug: Solifenacin Oral Tablet|Drug: Mirabegron 25mg Overactive Bladder Syndrome Far Eastern Memorial Hospital April 30 2021 --
NCT04641975 Recruiting Drug: Mirabegron|Drug: Placebo Overactive Bladder (OAB)|Pharmacokinetics of Mirabegron Astellas Pharma Global Development Inc.|Astellas Pharma Inc April 12 2021 Phase 3
NCT04693897 Not yet recruiting Drug: Mirabegron 50 MG|Drug: Solifenacin Succinate 5 MG Overactive Bladder Syndrome|Detrusor Overactivity Chang Gung Memorial Hospital March 1 2021 --
NCT04503850 Not yet recruiting Drug: Mirabegron 50 MG|Drug: Alpha Blockers Males With Benign Prostatic Hyperplasia Symptoms Kasr El Aini Hospital October 1 2020 --
NCT04501640 Completed Drug: mirabegron Pharmacokinetics of Mirabegron|Food Effect|Healthy Chinese Subjects Astellas Pharma China Inc.|Astellas Pharma Inc September 21 2020 Phase 4
NCT04286152 Recruiting Drug: Mirabegron 50 MG|Drug: Placebo oral tablet Nephrolithiasis Unity Health Toronto|Canadian Urological Association February 3 2020 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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