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阿罗洛尔 /Arotinolol {[allProObj[0].p_purity_real_show]}

货号:A127295

Arotinolol is a blocker of both α- and β-receptor, and also acts as a β3 receptor agonist. It is used in the treatment of high blood pressure and essential tremor.

Arotinolol 化学结构 CAS号:68377-92-4
Arotinolol 化学结构
CAS号:68377-92-4
Arotinolol 3D分子结构
CAS号:68377-92-4
Arotinolol 化学结构 CAS号:68377-92-4
Arotinolol 3D分子结构 CAS号:68377-92-4
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Arotinolol 纯度/质量文件 产品仅供科研

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α1D-adrenoceptor, pKi: 5.1

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β1-adrenoceptor, pIC50: 5.1

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97%
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adrenoceptor α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

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Prazosin HCl 95%
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Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

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β2-adrenergic receptor, Ki: 0.7nM

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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。

Arotinolol 生物活性

描述 Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol(30 mg/kg/d) relaxed vascular rings and the relaxations were attenuated by Nω-nitro-L-arginine methyl ester (L-NAME, NO synthase inhibitor) and the absence of endothelium[3]. On the beta3-receptor, arotinolol was a very weak (EC50 approximately 20 mM) and only partial (approximately 50%) agonist, but arotinolol also demonstrated the properties of being a beta3-receptor antagonist with a pK(B) of 5.7[4].

Arotinolol 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
NCT01351636 Chronic Kidney Disease Phase 4 Unknown September 2018 China, Shanghai ... 展开 >> Nan Chen Shanghai, Shanghai, China, 200025 收起 <<
NCT02612298 Essential Hypertension Phase 4 Unknown December 2018 China ... 展开 >> China PLA General Hospital Recruiting Beijing, China, 100039 Contact: Yundai Chen, MD          Contact: Yundai Chen, MD    +86 010 55499209    cyundai@medmail.com.cn 收起 <<

Arotinolol 参考文献

[1]Qian Z, Xu Y, et al. Enantiospecific determination of arotinolol in rat plasma by LC-MS/MS: application to a stereoselective pharmacokinetic study. J Pharm Biomed Anal. 2015 Jan;102:299-304.

[2]Sakanashi M, Miyamoto Y, et al. Effects of a new beta-adrenoceptor blocking agent, S-596 (arotinolol), on isolated dog coronary arteries. Arch Int Pharmacodyn Ther. 1983 Jun;263(2):208-16.

[3]Zhou W, Hong M, Zhang K, Chen D, Han W, Shen W, Zhu D, Gao P. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats. PLoS One. 2014 Feb 12;9(2):e88722.

[4]Zhao J, Golozoubova V, Cannon B, Nedergaard J. Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes. Can J Physiol Pharmacol. 2001 Jul;79(7):585-93. PMID: 11478592.

Arotinolol 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.91mL

5.38mL

2.69mL

Arotinolol 技术信息

CAS号68377-92-4
分子式C15H21N3O2S3
分子量 371.541
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 120 mg/mL(322.98 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

动物实验配方
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