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    Mirabegron (YM178)
    Mirabegron (YM178)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1098
    CAS #: 223673-61-8Purity ≥98%

    Description: Mirabegron (formerly YM-178; YM178; Myrbetriq; Betanis; Betmiga) is a potent and selective β3-adrenoceptor agonist with similar effects to antimuscarinic medications. It activates β3-adrenoceptor with an EC50 of 22.4 nM. Mirabegron is an approved drug for the treatment of overactive bladder. Mirabegron activates the β3 adrenergic receptor in the detrusor muscle in the bladder, which leads to muscle relaxation and an increase in bladder capacity.

    References: J Pharmacol Exp Ther. 2007 May;321(2):642-7; Xenobiotica. 2012 Dec;42(12):1187-96.

    Related CAS: 1215807-38-7 (Mirabegron D5)

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    Molecular Weight (MW)396.51
    FormulaC21H24N4O2S
    CAS No.223673-61-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 79 mg/mL (199.2 mM)
    Water:<1 mg/mL
    Ethanol: 8 mg/mL (20.17 mM)
    Solubility (In vivo)

    Chemical Name: 2-(2-Amino-1,3-thiazol-4-yl)-N-[4-(2-{[(2R)-2-hydroxy-2-phenylethyl]amino}ethyl)phenyl]acetamide

    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

    SMILES Code: O=C(NC1=CC=C(CCNC[[email protected]](O)C2=CC=CC=C2)C=C1)CC3=CSC(N)=N3

    SynonymsYM 178; Mirabegron; Myrbetriq; YM-178; YM178; Betanis; Betmiga


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    In 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 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,


    Cell Assay: CHO cells (105) are seeded in each well of a 24-well culture plate and subcultured. Three days later, the medium is exchanged with 250 μL/well Hanks' balanced salt solution containing 0.1 mM 3-isobutyl-1-methylxanthine, pH 7.4. The cells are incubated with each compound (isoproterenol, Mirabegron, BRL37344, and CL316,243 at final concentrations of 10-10 to 10-4 M) for 10 min at 37°C, after which incubation is stopped by the addition of 250 μL of 0.2 M HCl. cAMP concentration in the reaction mixture is measured by radioimmunoassay using an 125I-cAMP assay system using a gamma counter. Fifty microliters of reaction mixture is incubated with 50 μL of succinyl agent for 10 min at room temperature, after which the reaction is stopped by the addition of 400 μL of buffer solution. Fifty microliters of succinylated sample is incubated with 50 μL of 125I-cAMP and 50 μL of anti-cAMP antibody for 24 h at 4°C. At the end of the incubation period, 250 μL of charcoal suspension is added and centrifuged for 10 min at 2800g at 4°C. Two hundred and fifty microliters of supernatant is transferred into a tube and counted for 1 min using a gamma counter. The intrinsic activity (I.A.) relative to isoproterenol for each β-adrenoceptor agonist is calculated using the maximal response of each compound.

    In VivoMirabegron 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. 
    Animal modelRats
    Formulation & DosageMale (350 to 400 g) and female (225 to 290 g) Wistar rats are used. 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 are used in this study.
    References

    J Pharmacol Exp Ther. 2007 May;321(2):642-7; Xenobiotica. 2012 Dec;42(12):1187-96.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    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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