化学信息：
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化学名
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4-[2-[[7-amino-2-(furan-2-yl)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl]amino]ethyl]phenol
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简称
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ZM241385
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别名
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ZM 241385, ZM-241385
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中文名
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N/A
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化学式
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C16H15N7O2
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分子量
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337.34
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CAS号
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139180-30-6
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO67mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入1.48ml DMSO，或者每3.37mg加入1ml DMSO，配制成10mM溶液。SD2407-10mM用DMSO配制。
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生物信息：
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产品描述
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ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.
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信号通路
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GPCR & G Protein
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靶点
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adenosine A2A receptor
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－
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－
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－
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－
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IC50
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－
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－
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－
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－
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－
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体外研究
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ZM 241385 has high affinity for A2a receptors. In rat phaeochromocytoma cell membranes, ZM 241385 displaces binding of tritiated 5'-N-ethylcarboxamidoadenosine (NECA) with a pIC50 of 9.52. ZM241385 delays the appearance of anoxic depolarization (AD), a phenomenon strictly related to cell damage and death, protect from the synaptic activity depression brought about by a severe (7 min) OGD period, and protect CA1 neuron and astrocyte from injury.
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体内研究
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ZM-241385 significantly blunts the hypotensive effects of CCPA and NECA without altering the bradycardia induced by these agonists. It blocks the infarct size-reducing effects(cardioprotective effects) of this two distinct adenosine receptor agonists.
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临床实验
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N/A
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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PC12 cells
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浓度
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1μM
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处理时间
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24h
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方法
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Nitric oxide (NO) production is assessed by measuring the amount of nitrite, a stable metabolic product of NO that provides an indirect measurement of NO, by using the Griess diazotization reaction. Briefly, 24h after incubation with 1.0μM CG21680 or 1.0μM ZM241385 or exposure to SMF, samples of medium (150μl) are collected from cells and mixed with 130μl dH2O and with 20μl Griess reagent using instruction supplied by the manufacturer. After a 30 min incubation period at room temperature, the samples are evaluated spectrophotometrically at 548nM and OD values-in comparison with a standard curve is determined in culture medium by using serial dilutions of sodium nitrite-represented total stable metabolites of NO.
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动物实验
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动物模型
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Adult Sprague-Dawley rats
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配制
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10% DMSO in 1ml normal saline
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剂量
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1.5mg/kg
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给药方式
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i.v.
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参考文献：
1. Lasley RD, et al. Am J Physiol Heart Circ Physiol. 2007, 292(1):H426-31.
2. Wang Z, et al. PLoS One. 2010, 5(11):e13883.
3. S. M. Poucher, et al. Br J Pharmacol. 1995, 115(6), 1096-1102.
4. Pedata F, et al. Mediators Inflamm. 2014, 805198.
包装清单：
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产品编号
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产品名称
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包装
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SD2407-10mM
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ZM241385 (Adenosine Receptor抑制剂)
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10mM×0.2ml
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SD2407-5mg
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ZM241385 (Adenosine Receptor抑制剂)
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5mg
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SD2407-25mg
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ZM241385 (Adenosine Receptor抑制剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品对人体有毒，操作时请特别小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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