Mirabegron

Biological Activity

Mirabegron is a potent and selective β₃-adrenoceptor agonist (EC₅₀ = 22.4 nM). Displays >440-fold selectivity for β₃ over β₁ and β₂ adrenoceptors. Increases cAMP concentration in CHO cells expressing human β₃-adrenoceptor. Displays relaxant effect in ex vivo rat bladder muscle preparation precontracted with carbachol (Cat. No. 2810). Decreases frequency of bladder contraction in rats. Also promotes browning of white adipose tissue, reduces body weight, and improves glucose tolerance and insulin sensitivity in mice fed a high fat diet.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective β₃-adrenoceptor agonist, on bladder function.
   Takasu et al.
   J.Pharmacol.Exp.Ther., 2007;321:642
2. Beneficial metabolic effects of mirabegron in vitro and in high-fat diet-induced obese mice.
   Hao et al.
   J.Pharmacol.Exp.Ther., 2019;369:419
3. Bladder drug mirabegron exacerbates atherosclerosis through activation of brown fat-mediated lipolysis.
   Sui et al.
   Proc.Natl.Acad.Sci.U.S.A., 2019;116:10937

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