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ICI-118,551

ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist. ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor. The compound was developed by Imperial Chemical Industries, which was acquired by AkzoNobel in 2008.

目录号
EY6007
纯度
98%
规格
10 mg
原价
5200.00
售价
5200.00
库存
现货
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  • 生物活性

    ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β2 adrenergic receptor, as few other specific antagonists for this receptor are known. When dissolved in saline, the compound crosses the blood–brain barrier. Common systemic doses used in rodent research are 0.5 or 1mg/kg although efficacy has been demonstrated at doses as low as 0.0001mg/kg in rhesus monkeys. Doses up to 20mg/kg have been used without toxicity. At room temperature in saline, the ICI 118,551 hydrochloride is soluble to at least 2.5mg/mL.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Balaji Selvam,et.al. Comparison of Dynamics of Extracellular Accesses to the β1 and β2 Adrenoceptors Binding Sites Uncovers the Potential of Kinetic Basis of Antagonist Selectivity. Chem Biol Drug Des. Author manuscript; available in PMC 2013 Aug 1. Published in final edited form as: Chem Biol Drug Des. 2012 Aug; 80(2): 215–226. Published online 2012 May 2. doi: 10.1111/j.1747-0285.2012.01390.x.

    分子式
    C17H28ClNO2    		 分子量
    313.86    		 CAS号
    72795-19-8    		 储存方式
    -20 ℃ 长期保存2年。 冰袋运输。
    溶剂（常温）
    		 DMSO
    		 Water
    		 Ethanol

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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