Mirabegron

Catalog No.S4009 Synonyms: YM 178

Mirabegron Chemical Structure

Molecular Weight(MW): 396.51

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

Size Price Stock Quantity  
In DMSO USD 430 In stock
USD 270 In stock
USD 997 In stock
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Biological Activity

Description Mirabegron 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

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 powder
in solvent
Synonyms YM 178

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02981459 Withdrawn Urinary Frequency/Urgency|Bladder Irritable|Bladder Pain Syndrome State University of New York at Buffalo|Astellas Pharma Inc December 8 2017 Phase 4
NCT03106623 Completed Overactive Bladder Ono Pharmaceutical Co. Ltd April 7 2017 Phase 2
NCT02811289 Completed Type 2 Diabetes Université de Sherbrooke August 5 2016 Not Applicable
NCT02386072 Completed Urinary Bladder Overactive|Overactive Bladder|Urinary Bladder Diseases|Urologic Diseases Astellas Scientific & Medical Affairs Inc.|Astellas Pharma Inc January 5 2015 --
NCT01972841 Completed Urinary Bladder Overactive|Urinary Bladder Diseases\Urologic Diseases|Overactive Bladder|Urgency Incontinence Astellas Pharma Europe B.V.|Astellas Pharma Inc November 5 2013 Phase 3
NCT01898624 Completed Overactive Bladder Astellas Pharma Inc December 4 2012 --

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Adrenergic Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID