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Chemical Structure| 72795-01-8 同义名 : ICI-118551 Hydrochloride; ICI 118551 (hydrochloride)
CAS号 : 72795-01-8
货号 : A136388
分子式 : C17H28ClNO2
纯度 : 98%
分子量 : 313.86
MDL号 : MFCD00153812
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
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
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].
实验方案
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
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.