化合物ZD7288 T7516

Product Introduction
Bioactivity


英文名: ZD7288

描述: ZD7288 (ICI D7288) 是一种选择性超极化激活的环核苷酸门控通道阻滞剂，可抑制海马突触可塑性。

细胞实验: Cultured hippocampal neurons were incubated with 1 μM Fura-2 acetoxy-methylol ester for 30 minutes at 37°C, washed three times with artificial cerebrospinal fluid (containing 140 mM NaCl, 5 mM KCl, 2 mM CaCl2, 1 mM MgCl2, 10 mM glucose and 10 mM hydroxyethyl piperazine ethanesulfonic acid, pH 7.3), and then incubated at room temperature in the dark for 30 minutes.?Fura-2 fluorescence was observed by a Ratio Vision digital fluorescence microscopy system.?Fluorescence signals were evoked by 340 and 380 nm excitation wavelengths and collected at 510 nm by TILLvisION 4.0 software.?The 340:380 nm fluorescence ratio was used to represent [Ca2+]i.?Peak calcium change was represented as the percentage increase from baseline.?Neurons were incubated in ZD7288 (25, 50 or 100 μM) or 8-Br-cAMP (5 or 50 μM) for 15 minutes prior to stimulation with 50 μM glutamate.?All experiments were repeated in triplicate, using different batches of cells across 4–5 dishes[1].

体外活性: ZD7288 attenuated glutamate-induced rises in [Ca(2+)]i in a concentration-dependent manner and reversed 8-Br-cAMP-mediated facilitation of these glutamate-induced [Ca(2+)]i rises.?ZD7288 inhibits hippocampal synaptic plasticity both glutamate release and resultant [Ca(2+)]i increases in rat hippocampal neurons[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (170.76 mM)
H2O : 50 mg/mL (170.76 mM)


关键字: inhibit | Hyperpolarization activated cyclic nucleotide gated channels | ICI D-7288 | ICI D 7288 | HCN Channel | ZD-7288 | ZD7288 | ZD 7288 | Inhibitor

相关产品: Zatebradine hydrochloride | Cilobradine hydrochloride

相关库: Ion Channel Inhibitor Library | Anti-Hypertension Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Inhibitor Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途