Mirabegron

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Chemical Structure| 223673-61-8 同义名 : YM178
CAS号 : 223673-61-8
货号 : A187814
分子式 : C21H24N4O2S
纯度 : 98%
分子量 : 396.51
MDL号 : MFCD11100356
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(264.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 β3-AR is a G protein-coupled receptor. Functional β3-AR-mediated responses have been observed in human brown and white fat cells, where they mediate lipolysis; and in gall bladder, stomach, small intestine, prostate, colon, and bladder, where they evoke relaxation. Mirabegron is a selective β3-adrenoceptor agonist. Mirabegron concentration-dependently increased the accumulation of cAMP in CHO cells expressing human β3-ARs, with an EC50 value and I.A. of 22.4 nM and 0.8, respectively. Mirabegron concentration-dependently relaxed rat bladder smooth muscle strips precontracted with 10-6 M CCh with EC50 value of 5.1 μM. The maximal relaxant effect of mirabegron was 94.0±1.0%, that of CCh, indicating that mirabegron acts a full agonist in the rat bladder. Mirabegron concentration-dependently relaxed human bladder smooth muscle strips precontracted with 10-7 M CCh with EC50 value of 0.78 μM. The maximal relaxant effect of mirabegron was 89.4±2.3%. Mirabegron produced a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats[3]. SAAs (single-unit afferent activities) of both Aδ-fibers and C-fibers in response to bladder filling significantly decreased after mirabegron administration in a dose-dependent manner (Nerves with conduction velocities (CVs) >2.5 m/s were designated as Aδ-fibers, and nerves with CVs<2.5 m/s were designated as C-fibers)[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00337090 Overactive Bladder Phase 2 Completed - -
NCT02811289 Type 2 Diabetes Not Applicable Completed - Canada, Quebec ... 展开 >> centre de recherche du CHUS Sherbrooke, Quebec, Canada, J1H 5N4 收起 <<
NCT01043666 Urinary Bladder, Overactive Phase 3 Completed - China ... 展开 >> Beijing, China Dalian, China Fuzhou, China Guangzhou, China Hangzhou, China Hubei, China Hunan, China Jiangsu, China Liaoning, China Nanjing, China Shanghai, China India Ahmedabad, India Gurgaon, India Jaipur, India Lucknow, India New Delhi, India Pune, India Korea, Republic of Busan, Korea, Republic of Chungcheong Namdo, Korea, Republic of Daegu, Korea, Republic of Daejeon, Korea, Republic of Gwangju, Korea, Republic of Gyeonggi, Korea, Republic of Incheon, Korea, Republic of Jeollabuk, Korea, Republic of Jeollanam, Korea, Republic of Kyonggi, Korea, Republic of Seoul, Korea, Republic of Taiwan Chia-Yi, Taiwan Hualien, Taiwan Kaohsiung, Taiwan Taichung, Taiwan Tainan, Taiwan Taipei, Taiwan Taoyuan, Taiwan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.22mL

5.04mL

2.52mL
参考文献

[1]Takusagawa S, Miyashita A, et al. In vitro inhibition and induction of human cytochrome P450 enzymes by mirabegron, a potent and selective β3-adrenoceptor agonist. Xenobiotica. 2012 Dec;42(12):1187-96.

[2]Takasu T, Ukai M, 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. J Pharmacol Exp Ther. 2007 May;321(2):642-7.

[3]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. J Pharmacol Exp Ther. 2007;321(2):642‐647

[4]Aizawa N, Homma Y, Igawa Y. Effects of mirabegron, a novel β3-adrenoceptor agonist, on primary bladder afferent activity and bladder microcontractions in rats compared with the effects of oxybutynin. Eur Urol. 2012;62(6):1165‐1173