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G蛋白偶联受体/G蛋白
神经信号通路 内分泌学/激素
/ 肾上腺素能受体 / Mirabegron/米拉贝隆

Mirabegron/米拉贝隆 {[allProObj[0].p_purity_real_show]}

货号：A187814 同义名： YM178

Mirabegron是一种 β3 肾上腺素受体激动剂，EC50 值为 22.4 nM，用于治疗膀胱过度活跃症。

Mirabegron/米拉贝隆 化学结构 CAS号：223673-61-8
Mirabegron/米拉贝隆 化学结构
CAS号：223673-61-8
Mirabegron/米拉贝隆 3D分子结构
CAS号：223673-61-8
Mirabegron/米拉贝隆 化学结构 CAS号：223673-61-8
Mirabegron/米拉贝隆 3D分子结构 CAS号：223673-61-8
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Mirabegron/米拉贝隆 纯度/质量文件 产品仅供科研

货号：A187814 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ 98%
Maprotiline HCl ✔ 98%
Cisatracurium besylate ✔ 96%
Yohimbine HCI ✔ 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

 		+

β1-adrenoceptor, pIC50: 5.1

 		97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

 		97%
Piribedil ++

adrenoceptor α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

 		98%
Prazosin HCl ✔ 95%
Silodosin ✔ 98%
Phenoxybenzamine HCl ✔ 98%
Labetalol HCl ✔ 98+%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

 		98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		99%
Alfuzosin HCl ✔ 98%
Terazosin HCl ✔ 99%
Atipamezole ✔ 95%
Phentolamine methanesulfonate salt ✔ 99%
Carvedilol ✔ 99%
Doxazosin mesylate ✔ 99%
Tolazoline HCl ✔ 98%
Esmolol HCl ✔ 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

 		99%
Zenidolol HCl ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

 		98%
Acebutolol HCl ✔ 97+%
Carteolol HCl ✔ 98+%
Betaxolol ✔ 99%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

 		97%
Bisoprolol ✔ 97%
Sotalol HCl ✔ 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

 		99%
Metoprolol ✔ 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Mirabegron/米拉贝隆 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].

Mirabegron/米拉贝隆 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 <<

Mirabegron/米拉贝隆 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

Mirabegron/米拉贝隆 实验方案

计算器
存储液制备 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

Mirabegron/米拉贝隆 技术信息

CAS号223673-61-8
分子式C21H24N4O2S
分子量 396.51
SMILES Code O=C(NC1=CC=C(CCNC[C@H](O)C2=CC=CC=C2)C=C1)CC3=CSC(N)=N3
MDL No. MFCD11100356
别名 YM178
运输蓝冰
InChI Key PBAPPPCECJKMCM-IBGZPJMESA-N
Pubchem ID 9865528
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

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

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Mirabegron | YM178 | Adrenergic Receptor | AmBeed-信号通路专用抑制剂 | Mirabegron/米拉贝隆 纯度/质量文件 | Mirabegron/米拉贝隆 亚型比较 | Mirabegron/米拉贝隆 生物活性 | Mirabegron/米拉贝隆 临床数据 | Mirabegron/米拉贝隆 参考文献 | Mirabegron/米拉贝隆 实验方案 | Mirabegron/米拉贝隆 技术信息

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