Home Neuronal Signaling Adrenergic Receptor agonist Mirabegron For research use only.

Mirabegron

Synonyms: YM 178

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

Mirabegron Chemical Structure

Mirabegron Chemical Structure

CAS: 223673-61-8

Selleck's Mirabegron has been cited by 12 publications

Purity & Quality Control

Batch: S400901 DMSO] 79 mg/mL] false] Ethanol] 8 mg/mL] false] Water] Insoluble] false Purity: 99.8%
99.8

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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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05621616 Recruiting Neurogenic Detrusor Overactivity Astellas Pharma Global Development Inc.|Astellas Pharma Inc June 26 2023 Phase 3
NCT05040984 Recruiting Overactive Bladder Syndrome Far Eastern Memorial Hospital April 30 2021 --
NCT04641975 Terminated Overactive Bladder (OAB)|Pharmacokinetics of Mirabegron Astellas Pharma Global Development Inc.|Astellas Pharma Inc March 15 2021 Phase 3
NCT04693897 Unknown status Overactive Bladder Syndrome|Detrusor Overactivity Chang Gung Memorial Hospital March 1 2021 --

Chemical lnformation & Solubility

Molecular Weight 396.51 Formula

C21H24N4O2S
CAS No. 223673-61-8 SDF Download Mirabegron SDF
Smiles C1=CC=C(C=C1)C(CNCCC2=CC=C(C=C2)NC(=O)CC3=CSC(=N3)N)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (199.23 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble


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In vivo
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