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Zenidolol hydrochloride {[allProObj[0].p_purity_real_show]}

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.

Zenidolol hydrochloride 化学结构 CAS号:72795-01-8
Zenidolol hydrochloride 化学结构
CAS号:72795-01-8
Zenidolol hydrochloride 3D分子结构
CAS号:72795-01-8
Zenidolol hydrochloride 化学结构 CAS号:72795-01-8
Zenidolol hydrochloride 3D分子结构 CAS号:72795-01-8
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Zenidolol hydrochloride 纯度/质量文件 产品仅供科研

货号:A136388 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Zenidolol hydrochloride 生物活性

靶点
  • β-adrenergic receptor

    β1-adrenergic receptor, Ki:611nM

    β2-adrenergic receptor, Ki:0.7nM

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].

Zenidolol hydrochloride 参考文献

[1]Wenzel D, Knies R, et al. beta(2)-adrenoceptor antagonist ICI 118,551 decreases pulmonary vascular tone in mice via a G(i/o) protein/nitric oxide-coupled pathway. Hypertension. 2009 Jul;54(1):157-63.

[2]Yasuda G, Sun L, et al. The beta 1- and beta 2-adrenoceptor subtypes in cultured rat inner medullary collecting duct cells. Am J Physiol. 1996 Sep;271(3 Pt 2):F762-9.

[3]Yasuda G, Sun L, Lee HC, Umemura S, Jeffries WB. The beta 1- and beta 2-adrenoceptor subtypes in cultured rat inner medullary collecting duct cells. Am J Physiol. 1996 Sep;271(3 Pt 2):F762-9. doi: 10.1152/ajprenal.1996.271.3.F762. PMID: 8853440.

[4]Gong H, Sun H, Koch WJ, Rau T, Eschenhagen T, Ravens U, Heubach JF, Adamson DL, Harding SE. Specific beta(2)AR blocker ICI 118,551 actively decreases contraction through a G(i)-coupled form of the beta(2)AR in myocytes from failing human heart. Circulation. 2002 May 28;105(21):2497-503. doi: 10.1161/01.cir.0000017187.61348.95. PMID: 12034656.

[5]Wenzel D, Knies R, Matthey M, Klein AM, Welschoff J, Stolle V, Sasse P, Röll W, Breuer J, Fleischmann BK. beta(2)-adrenoceptor antagonist ICI 118,551 decreases pulmonary vascular tone in mice via a G(i/o) protein/nitric oxide-coupled pathway. Hypertension. 2009 Jul;54(1):157-63. doi: 10.1161/HYPERTENSIONAHA.109.130468. Epub 2009 May 26. PMID: 19470879.

Zenidolol hydrochloride 实验方案

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

Zenidolol hydrochloride 技术信息

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

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