货号:A136388 同义名: ICI-118551 Hydrochloride;ICI 118551 (hydrochloride)
ICI 118551 HCl is a selective and inverse β2 adrenergic receptor antagonist with Ki values of 1.2, 120 and 257nM for β2, β1 and β3 receptors, respectively.
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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 | ✔ | 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 α2A, pKi: 7.1 adrenoceptor α2C, pKi: 7.2 |
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 |
99% | |||||||||||||||||
Alfuzosin HCl | ✔ | 98% | |||||||||||||||||
Terazosin HCl | ✔ | 99% | |||||||||||||||||
Atipamezole | ✔ | 95% | |||||||||||||||||
Phentolamine methanesulfonate salt | ✔ | 99% | |||||||||||||||||
Doxazosin mesylate | ✔ | 99% | |||||||||||||||||
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。 |
靶点 |
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描述 | ICI 118551 (Hydrochloride) is a highly selective β2 adrenergic receptor antagonist. ICI 118551 inhibits cAMP accumulation by 50% with IC50 of 1.7 μM in IMCD cells[3].ICI 118551 decreased contraction in ventricular myocytes from failing human hearts by 45.3+/-4.1% but had little effect in nonfailing hearts. ICI 118551 effectively acts as an agonist at the G(i)-coupled beta(2)AR(adrenoceptor), producing a direct negative inotropic effect[4]. Moreover,ICI 118551 evoked a decrease of vascular tone in large pulmonary arteries and reduced the sensitivity of pulmonary arteries toward different contracting agents, eg, norepinephrine, serotonin, or endothelin[5]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.19mL 0.64mL 0.32mL |
15.93mL 3.19mL 1.59mL |
31.86mL 6.37mL 3.19mL |
CAS号 | 72795-01-8 |
分子式 | C17H28ClNO2 |
分子量 | 313.863 |
别名 | ICI-118551 Hydrochloride;ICI 118551 (hydrochloride) |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Room Temperature |
溶解度 |
DMSO: 35 mg/mL(111.51 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 H2O: 8 mg/mL(25.49 mM),配合低频超声助溶 |
动物实验配方 |