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仪器信息网试剂标物生化试剂生物分子 ICI-118551

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爱必信(上海)生物科技有限公司

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ICI-118551

价格：￥ 1337

品牌：爱必信

供货周期：一周

货号：abs816198

CAS：1217094-53-5

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抑制剂描述：

产品名称：ICI-118551

产品别名：见爱必信官网

英文别名：ICI-118551

靶点：Adrenergic Receptor

CAS：1217094-53-5

纯度：

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：ICI-118551 is a highly selective <b>β2-adrenergic receptor antagonist</b> with <b>Ki</b> values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

溶解性：体外:
DMSO 62mg/mL(197.54mM)
Ethanol 62mg/mL(197.54mM)
Water 21mg/mL(66.9mM)

体外研究：

ICI-118551 inhibits cAMP accumulation by 50% (IC50 = 1.7 mM). Pharmacological experiments proves that the right shift of the norepinephrine dose-response curve by ICI 118551 is mediated via a beta(2)-adrenoceptor/G(i/o) protein-dependent pathway enhancing NO production in the endothelium; these results are corroborated in beta-adrenoceptor and endothelial NO synthase knockout mice where ICI 118551 has no effect. ICI 118551 increases vascular lumen diameter in lung sections and reduces pulmonary arterial pressure under normoxia and under hypoxia in the isolated perfused lung model. Transgenic mice with high beta(2)AR number and increased G(i) levels have normal basal contractility but show a similar negative inotropic response to ICI 118,551. Overexpression of human beta(2)AR in rabbit myocytes using adenovirus potentiates the negative inotropic effect of ICI 118,551. In human, rabbit, and mouse myocytes, the negative inotropic effects are blocked after treatment of cells with pertussis toxin to inactivate G(i), and overexpression of G(i)alpha(2) induces the effect de novo in normal rat myocytes.

体内研究：After 1 week of treatment, ICI 118,551 has no effect on the beta 1-receptor mediated shortening of electromechanical systole (QS2I), the rise in systolic pressure and rise in renin, whereas these responses are blocked by a dose factor of eight after propranolol. ICI 118,551 and propranolol equally block the beta 2-receptor mediated fall in diastolic pressure and the rise in noradrenaline. beta 2-selective blockade by ICI 118,551 lowers blood pressure.

产品信息订购：

产品货号	产品名称	规格	价格	大包装及货期
abs816198	ICI-118551	5mg	1337.00	立即咨询
abs816198	ICI-118551	25mg	4088.00	立即咨询
abs816198	ICI-118551	100mg	9591.00	立即咨询

产品更多信息请进入爱必信网站咨询

生化试剂 ICI-118551由爱必信(上海)生物科技有限公司为您提供，如想了解更多关于生物分子 ICI-118551的报价、规格、厂家等信息，欢迎来电或留言咨询。除供应ICI-118551外，爱必信(上海)生物科技有限公司还可为您提供：

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