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Submit ReviewMirabegron 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.
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分子量 | 396.51 |
公式 | C21H24N4O2S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 223673-61-8 |
PubChem ID | 9865528 |
InChI Key | PBAPPPCECJKMCM-IBGZPJMESA-N |
Smiles | NC1=NC(CC(=O)NC2=CC=C(CCNC[C@H](O)C3=CC=CC=C3)C=C2)=CS1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 39.65 | 100 | |
ethanol | 7.93 | 20 |
以下数据基于产品分子量 396.51。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.52 mL | 12.61 mL | 25.22 mL |
5 mM | 0.5 mL | 2.52 mL | 5.04 mL |
10 mM | 0.25 mL | 1.26 mL | 2.52 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
参考文献是支持产品生物活性的出版物。
Takasu et al (2007) 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. J.Pharmacol.Exp.Ther. 321 642 PMID: 17293563
Hao et al (2019) Beneficial metabolic effects of mirabegron in vitro and in high-fat diet-induced obese mice. J.Pharmacol.Exp.Ther. 369 419 PMID: 30940691
Sui et al (2019) Bladder drug mirabegron exacerbates atherosclerosis through activation of brown fat-mediated lipolysis. Proc.Natl.Acad.Sci.U.S.A. 116 10937 PMID: 31085638
If you know of a relevant reference for Mirabegron, please let us know.
关键词: Mirabegron, Mirabegron supplier, YM178, YM, 178, potent, selective, beta3, adrenoceptor, adrenergic, receptor, agonists, agonism, bladder, relaxant, atherosclerotic, B3, Adrenergic, Beta-3, Receptors, 7070, Tocris Bioscience
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.