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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* 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
NCT03049462 Recruiting Healthy Volunteers National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) January 30, 2017 Phase 1
NCT02981459 Not yet recruiting Urinary Frequency/Urgency|Bladder Irritable|Bladder Pain Syndrome State University of New York at Buffalo|Astellas Pharma Inc January 2017 Phase 4
NCT02279615 Not yet recruiting Overactive Bladder|Benign Prostatic Hyperplasia St. Josephs Healthcare Hamilton December 2016 Phase 4
NCT02893553 Recruiting Spinal Cord Injury|Autonomic Dysreflexia|Baroreceptor Integrity|Sympathetic Integrity|Vagal Integrity|Autonomic Integrity|Hypotensive|Cognitive Function|Cerebral Blood Flow|Blood Pressure James J. Peters Veterans Affairs Medical Center|Kessler Foundation December 2016 Phase 2
NCT02744430 Not yet recruiting Ureteral Obstruction|Flank Pain Baylor College of Medicine November 2016 Phase 2
NCT02916693 Not yet recruiting Erectile Dysfunction|Overactive Bladder|Urinary Incontinence Johns Hopkins University|Astellas Pharma US, Inc. September 2016 Phase 1|Phase 2

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Adrenergic Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID