Name: Mirabegron
Brand: Selleck Chemicals
SKU: S4009
Rating: 5 (14 reviews)

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.8

Related Targets	AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Adrenergic Receptor Inhibitors	ICI 118551 Hydrochloride (Zenidolol) L755507 Yohimbine HCl Atipamezole Naftopidil Detomidine HCl Higenamine hydrochloride Adrenalone HCl Medetomidine HCl Deoxycorticosterone acetate

Chemical Information, Storage & Stability

Molecular Weight	396.51	Formula	C₂₁H₂₄N₄O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	223673-61-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	YM 178			Smiles	C1=CC=C(C=C1)C(CNCCC2=CC=C(C=C2)NC(=O)CC3=CSC(=N3)N)O

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (199.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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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.

Mechanism of Action

Targets/IC₅₀/Ki	β3-adrenoceptor 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. This compound has little agonistic effect on 1- and 2-ARs. It 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 this chemical are 94.0 % and 89.4% that of carbachol, respectively. It 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. This compound 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 anaesthetised rats. 3 mg/kg i.v. this compound suppresses the frequency to 2 counts/10 min. It does not decrease the amplitude of rhythmic bladder contraction. This chemical decreases primary bladder afferent activity and bladder microcontractions in rats. It (0.3 and 1 mg/kg) inhibits mechanosensitive single-unit afferent activities (SAAs) of Aδ fibres in response to bladder filling. SAAs of C-fibres decrease only at 1 mg/kg this compound treatment. Its administration suppresses the mean bladder pressure and the number of microcontractions during an isovolumetric condition of the bladder. It is efficient on facilitation of bladder storage. This compound dose-dependently decreases the resting intravesical pressure. It dose dependently decreases the frequency of nonvoiding contractions, considered an index of abnormal response in bladder storage. It exhibits no significant effects on the amplitude of nonvoiding contractions, micturition pressure, threshold pressure, voided volume, residual volume, or bladder capacity.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17293563/ [2] https://pubmed.ncbi.nlm.nih.gov/22834478/ [3] https://pubmed.ncbi.nlm.nih.gov/22981677/ [4] https://pubmed.ncbi.nlm.nih.gov/23224420/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05621616	Recruiting	Neurogenic Detrusor Overactivity	Astellas Pharma Global Development Inc.\|Astellas Pharma Inc	February 28 2024	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	--

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Mirabegron Adrenergic Receptor agonist

Chemical Structure

Molecular Weight: 396.51