Toggle Nav

Mirabegron (YM178)

Catalog No.
A8474
Selective β3-adrenoceptor agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$145.00
In stock
5mg
$130.00
In stock
10mg
$210.00
In stock
50mg
$470.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Mirabegron (YM178) is the first selective β3-adrenoceptor (β3-AR) agonist with EC50 value of 22.4 nM which is clinically effective for overactive bladder [1]. 

β3-AR, one of three β-adrenoceptors (β-AR) subtypes, is sparsely distributed in the humans, and functional responses regulated by have been discovered in human brown and white fat cells, and gall bladder, stomach, small intestine, prostate, colon, and bladder [1]. 

Mirabegron (YM178) exhibits significant selectivity for β-ARs. When tested with Chinese hamster ovary expressing human β-ARs, EC50 values of Mirabegron for β1-ARs, β2-ARs and β3-ARs were 22.4 nM, 10000 nM or more, respectively. The ratio of intrinsic activities of Mirabegron (YM178) versus maximal response induced by isoproterenol of nonselective β-AR agonist was 0.8 for human β3-AR, 0.1 for human β1-AR, and 0.1 for human β2-AR [1]. 

In anesthetized rats, Mirabegron (YM178) at a dose of 3 mg/kg i.v. reduced the frequency of rhythmic bladder contraction caused by intravesical filling with saline without inhibiting its amplitude. By contrast, Oxybutynin apparently raised the frequency of rhythmic bladder contraction and reduced its amplitude at doses of 0.272 mg/kg i.v. or more [1]. 

Reference:

[1]. Takasu T, Ukai M, Sato S, et al. 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. The Jounal of pharmacology and experimental therapeutic. 2007, 321(2):642-7.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt396.51
Cas No.223673-61-8
FormulaC21H24N4O2S
Solubility≥19.8mg/mL in DMSO
Chemical Name2-(2-amino-1,3-thiazol-4-yl)-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]acetamide
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)C(CNCCC2=CC=C(C=C2)NC(=O)CC3=CSC(=N3)N)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control