Mirabegron (YM178)

Alias: YM 178; Mirabegron; Myrbetriq; YM-178; YM178; Betanis; Betmiga
Cat No.:V1098 Purity: =99.39%
Mirabegron (formerly YM-178; YM178; Myrbetriq; Betanis; Betmiga) is a potent and selective β3-adrenoceptor agonist with similar effects to antimuscarinic medications.
Mirabegron (YM178) Chemical Structure CAS No.: 223673-61-8
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
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1g
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Other Forms of Mirabegron (YM178):

  • (Rac)-Mirabegron D5
Official Supplier of:
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Purity & Quality Control Documentation

Purity: =99.39%

Purity: ≥98%

Product Description

Mirabegron (formerly YM-178; YM178; Myrbetriq; Betanis; Betmiga) is a potent and selective β3-adrenoceptor agonist with similar effects to antimuscarinic medications. It stimulates the β3-adrenoceptor with an EC50 of 22.4 nM. The medication mirabegron is authorized for the management of overactive bladder. When the β3 adrenergic receptor in the bladder's detrusor muscle is activated by mirabegron, the muscle relaxes and the bladder's capacity increases.

Biological Activity I Assay Protocols (From Reference)
Targets
β3-adrenoceptor ( EC50 = 22.4 nM )
ln Vitro

In vitro activity: Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human 3-adrenoceptors (ARs) with I.A. of 0.8. Mirabegron barely affects 1- and 2-ARs agonistically. With EC50 values of 5.1 μM and 0.78 μM, respectively, mirabegron concentration-dependently relaxes rat and human bladder smooth muscle strips precontracted with 10-6 M or 10-7 M carbachol. Mirabegron's maximal relaxant effects are 94.0% and 89.4% of those of carbachol, respectively. Mirabegron is a time-dependent inhibitor of CYP2D6 in the presence of NADPH, as demonstrated by the fact that after 30 minutes of preincubation, the IC50 value in human liver microsomes dropped from 13 to 4.3 μM. Mirabegron inhibits CYP2D6 in part through an irreversible or quasi-irreversible metabolism-dependent mechanism.

ln Vivo
Mirabegron causes rats given anesthesia to experience a dose-dependent decrease in the frequency of rhythmic bladder contractions. 3 mg intravenously/kg. Mirabegron reduces the frequency to two counts per minute. Mirabegron does not lessen the rhythmic bladder contraction's amplitude. In rats, mirabegron reduces both bladder microcontractions and primary bladder afferent activity. Mechanosensitive single-unit afferent activities (SAAs) of Aδ fibers in response to bladder filling are inhibited by mirabegron (0.3 and 1 mg/kg). Only at 1 mg/kg of Mirabegron treatment do SAAs of C-fibers decrease. The administration of mirabegron suppresses both the mean bladder pressure and the number of microcontractions when the bladder is in an isovolumetric state. Mirabegron effectively aids in the storage of the bladder. In a dose-dependent manner, mirabegron lowers the intrathecal pressure at rest. Mirabegron reduces the frequency of non-voiding contractions dose-dependently, which is thought to be a sign of an aberrant response in bladder storage. Mirabegron shows no discernible effects on micturition pressure, threshold pressure, voided volume, residual volume, bladder capacity, or the amplitude of nonvoiding contractions.
Cell Assay
In every well of a 24-well culture plate, 105 CHO cells are deposited and allowed to grow. A pH 7.4 Hanks balanced salt solution containing 0.1 mM 3-isobutyl-1-methylxanthine is added to each well of the medium three days later. 250 μL of 0.2 M HCl is added to end the incubation of the cells after they have been exposed to each compound (isoproterenol, Mirabegron, BRL37344, and CL316,243) for 10 minutes at 37°C. The compounds are added at final concentrations of 10-10 to 10- M. Through radioimmunoassay with a 125I-cAMP assay system and a gamma counter, the concentration of cAMP in the reaction mixture is determined. The reaction is stopped by adding 400 μL of buffer solution after 50 microliters of reaction mixture and 50 μL of succinyl agent are incubated for 10 minutes at room temperature. For 24 hours at 4°C, 50 microliters of succinylated sample are incubated with 50 μL of 125I-cAMP and 50 μL of anti-cAMP antibody. After the incubation period, add 250 μL of charcoal suspension, and centrifuge at 2800g for 10 minutes at 4°C. After being transferred into a tube, 250 microliters of supernatant are counted for one minute using a gamma counter. The maximal response of each compound is used to calculate the intrinsic activity (I.A.) relative to isoproterenol for each β-adrenoceptor agonist.
Animal Protocol
It uses Wistar rats, both male (350–400 g) and female (225–290 g). In this investigation, the free-form doses of 0.03, 0.1, 0.3, 1, and 3 mg/kg for mirabegron and 0.0272, 0.0907, 0.272, 0.907, and 2.72 mg/kg for oxybutynin were employed.
Rats
References

[1]. Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. J Pharmacol Exp Ther. 2007 May;321(2):642-7.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H24N4O2S
Molecular Weight
396.51
Exact Mass
396.16
Elemental Analysis
C, 63.61; H, 6.10; N, 14.13; O, 8.07; S, 8.09
CAS #
223673-61-8
Appearance
Solid powder
SMILES
C1=CC=C(C=C1)[C@H](CNCCC2=CC=C(C=C2)NC(=O)CC3=CSC(=N3)N)O
InChi Key
PBAPPPCECJKMCM-IBGZPJMESA-N
InChi Code
InChI=1S/C21H24N4O2S/c22-21-25-18(14-28-21)12-20(27)24-17-8-6-15(7-9-17)10-11-23-13-19(26)16-4-2-1-3-5-16/h1-9,14,19,23,26H,10-13H2,(H2,22,25)(H,24,27)/t19-/m0/s1
Chemical Name
2-(2-amino-1,3-thiazol-4-yl)-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]acetamide
Synonyms
YM 178; Mirabegron; Myrbetriq; YM-178; YM178; Betanis; Betmiga
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 79~100 mg/mL (199.2~252.2 mM)
Water: <1 mg/mL
Ethanol: ~8 mg/mL (~20.2 mM)
Solubility (In Vivo)

Mirabegron (10 mg/ml) dissolved in DMSO (50%, vol%) and polyethylene glycol (50%, vol%)

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5220 mL 12.6100 mL 25.2200 mL
5 mM 0.5044 mL 2.5220 mL 5.0440 mL
10 mM 0.2522 mL 1.2610 mL 2.5220 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT06181019 Active
Recruiting
Drug: 50 mg of mirabegron
Combination Product: acupuncture
combined with mirabegron
Overactive Bladder The Affiliated Ganzhou Hospital
of Nanchang University
December 1, 2021 Phase 1
NCT05745584 Active
Recruiting
Drug: Mirabegron
(beta3-adrenoceptor agonist),
Anticholinergics
Patients With Low Bladder
Compliance of 20ml/H2O or
Less Despite Taking Anticholinergics
Yonsei University January 12, 2016 Not Applicable
NCT06011265 Active
Recruiting
Drug: Myrbetriq 25Mg Extended
-Release Tablet
Drug: Placebo
Thermoregulation Christopher Bell April 27, 2023 Early Phase 1
NCT05779514 Recruiting Drug: Mirabegron Tumour Zhejiang Provincial People's
Hospital
August 18, 2022 Not Applicable
NCT05051436 Recruiting Drug: Mirabegron 50 MG
Drug: Tadalafil 10 MG
Drug: Placebo
Pre-diabetes
Obesity
Philip Kern December 13, 2021 Phase 4
Biological Data
  • Mirabegron
    cAMP accumulation in CHO cells expressing human β1-AR (A), β2-AR (B), and β3-AR (C).J Pharmacol Exp Ther.2007 May;321(2):642-7.
  • Mirabegron
    Relaxing effect of isoproterenol, YM178, and CGP-12177A in rat bladder strips precontracted with carbachol.J Pharmacol Exp Ther.2007 May;321(2):642-7.
  • Mirabegron
    Relaxing effect of isoproterenol, YM178, and CGP-12177A in human bladder strips precontracted with carbachol.J Pharmacol Exp Ther.2007 May;321(2):642-7.
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