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.
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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 hydrochloride | ✔ | 98% | |||||||||||||||||
Cisatracurium besylate | ✔ | 98% | |||||||||||||||||
Yohimbine HCI | ✔ | 99+% | |||||||||||||||||
BMY 7378 |
++
α2C-adrenoceptor, pKi: 6.54 α1D-adrenoceptor, pKi: 5.1 |
+
β1-adrenoceptor, pIC50: 5.1 |
97% | ||||||||||||||||
Asenapine maleate |
++++
α2A-adrenergic receptor, pKi: 8.9 α2B-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% | |||||||||||||||||
Naftopidil |
+++
α1A-adrenergic receptor, Ki: 3.7 nM α1D-adrenergic receptor, Ki: 20 nM |
98% | |||||||||||||||||
Naftopidil 2HCl |
+
α1-adrenergic receptor, IC50: 0.2 μM |
97% | |||||||||||||||||
Alfuzosin HCl | ✔ | 98% | |||||||||||||||||
Terazosin HCl | ✔ | 99% | |||||||||||||||||
Atipamezole | ✔ | 95% | |||||||||||||||||
Phentolamine methanesulfonate salt | ✔ | 99% | |||||||||||||||||
Doxazosin mesylate | ✔ | 98% | |||||||||||||||||
Tolazoline HCl | ✔ | 98% | |||||||||||||||||
Zenidolol hydrochloride |
++++
β1-adrenergic receptor, Ki: 611nM β2-adrenergic receptor, Ki: 0.7nM |
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。 |
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]. |
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 << |
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 |
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 |