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Mirabegron(YM178)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Mirabegron(YM178)图片
CAS NO:223673-61-8
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt396.51
Cas No.223673-61-8
FormulaC21H24N4O2S
Solubilityinsoluble in H2O; ≥16.13 mg/mL in EtOH; ≥19.83 mg/mL in DMSO
Chemical Name2-(2-amino-1,3-thiazol-4-yl)-N-[4-[2-[[(2R)-2-hydroxy-2-phenylethyl]amino]ethyl]phenyl]acetamide
Canonical SMILESC1=CC=C(C=C1)C(CNCCC2=CC=C(C=C2)NC(=O)CC3=CSC(=N3)N)O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

Cell experiment:[1]

Cell lines

Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR)

Reaction Conditions

10-10~ 10-4M for 10 min incubation

Applications

Mirabegron concentration-dependently increased the accumulation of cyclic AMP (cAMP) in CHO cells expressing human β3-AR, with an EC50 value of 22.4 nM. Mirabegron had little agonistic effect on β1-AR and β2-AR, and did not induce cAMP elevation in untransfected CHO cells.

Animal experiment:[1]

Animal models

Male (350 to 400 g) and female (225 to 290 g) Wistar rats

Dosage form

3 mg/kg

Administered intravenously (i.v.)

Applications

Mirabegron at a dose of 3 mg/kg i.v. decreased the frequency of rhythmic bladder contraction induced by intravesical filling with saline without suppressing its amplitude in anesthetized rats. These findings suggest the suitability of mirabegron as a therapeutic drug for the treatment of symptoms of overactive bladder such as urinary frequency, urgency, and urge incontinence.

Note

The technical data provided above is for reference only.

References:

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. Journal of Pharmacology and Experimental Therapeutics, 2007, 321(2): 642-647.