Catalog No.S4009 Synonyms: YM 178
Molecular Weight(MW): 396.51
Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
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Choose Selective Adrenergic Receptor Inhibitors
|Description||Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.|
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.  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. 
|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.  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.  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. |
|In vitro||DMSO||79 mg/mL (199.23 mM)|
|Ethanol||8 mg/mL (20.17 mM)|
|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.
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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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