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ICI 118,551 hydrochloride  ≥98%

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包装规格：1mg 5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于水（12.5mg/mL 超声），溶于DMSO（25mg/mL 超声）
产品描述：基本信息 产品编号： I10603 产品名称： ICI 118,551 hydrochloride CAS: 72795-01-8   储存条件 粉末 -20℃ 四年     分子式： C17H28ClNO2 溶于液体 -80℃ 6个月 分子量： 313.86 -20℃ 1个月 化学名：  (2R,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-(propan-2-ylamino)butan-2-ol;hydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.1861mL 15.9307mL 31.8613mL 5mM 0.6372mL 3.1861mL 6.3723mL 10mM 0.3186mL 1.5931mL 3.1861mL   生物活性 产品描述 一种高度选择性的 β2 adrenergic receptor 拮抗剂，结合 β2，β1 和 β3 肾上腺素能受体的Ki 值分别为 0.7，49.5 和 611nM。 靶点 Ki:0.7nM (β2 receptor),49.5nM (β1 receptor),611nM (β3 receptor).   体外研究 ICI 118551 inhibits cAMP accumulation with IC50 of 1.7μM in IMCD cells.ICI 118551 (10μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO.In failing human heart,ICI 118551 has significant effects on beat duration,with time-to-peak contraction and time-to-90% relaxation reduced compared with basal contraction.Negative Inotropic Effect of ICI 118551 Is Not cAMP-Related.Overexpression of β2AR in rabbit myocytes enhances negative inotropic effects of ICI 118551. 体内研究 ICI 118551 (0.2mg/kg) injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure.   推荐实验方法(仅供参考) 激酶实验： One hour prior to assay,the growth media are removed from the wells and replaced with 50uL of Hanks’balanced salt solution that also contained 0.5mM of MgCl2•6H2O,0.4mM of MgSO4•7H2O,20mM of N-2-hydroxyethylpiperazine-N’-2ethanesulfonic acid (HEPES),1.2mM of 3-isobutyl-1-methylxanthine (IBMX),0.95mM of CaCl2,and 0.05% of BSA.Each plate is placed in a 37℃ shaking water bath for dose-response studies.In one study,various doses of isoproterenol (10-9-10-5M) and β1- and β2-receptor-selective partial agonists (tazolol,prenalterol,salbutamol,and terbutaline,10-6 and 10-5M,respectively) are added (5 wells/dose/plate) and incubated for 10 min.In another study,the cells are stimulated with 10μM isoproterenol in the presence or absence of various doses of β-adrenoceptor antagonists.The incubations are terminated after 10 min by the addition of 100μL of 10% trichloroacetic acid (TCA) (final TCA concentration of 5%).TCA is removed twice by extraction with H20-saturated ether, and samples are dried at 80℃ overnight,prior to resuspension in 50mM of sodium acetate buffer.The CAMP content is measured with a radioimmunoassay kit.
保存条件：-20℃

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