化学信息：
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化学名
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N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-4-chlorobenzamide
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简称
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PNU282987
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别名
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PNU 282987, PNU-282987
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中文名
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N/A
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化学式
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C14H18Cl2N2O
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分子量
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301.21
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CAS号
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123464-89-1
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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; DMSO61mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入1.66ml DMSO，或者每3.01mg加入1ml DMSO，配制成10mM溶液。SF9020-10mM用DMSO配制。
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生物信息：
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产品描述
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PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50≥60μM).
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信号通路
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Transmembrane Transporters; Neuronal Signaling
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靶点
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α7 nAChR agonist
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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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26nM(Ki)
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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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Treatment with PNU-282987 resulted in an attenuation of neuroinflammation in the MPTP-lesioned SN. Furthermore, PNU-282987 attenuated MPTP-induced dopaminergic cell loss in the SN and reduced striatal dopamine depletion.
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体内研究
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Mice were subjected to 70% partial hepatic I/R for 60 min and pretreated with either vehicle or with PNU-282987, and blood and hepatic tissue samples were collected at 3, 6 and 12h following reperfusion. pretreatment with PNU-282987 decreased serum transaminase levels and ameliorated liver injury after hepatic I/R. Moreover, pretreatment with PNU-282987 suppressed NF-κB activation, cytokine production (tumor necrosis factor α, interleukin 1β), and HMGB1 expression in liver after hepatic I/R. Mice treated with 2.5 and 10mg/kg of PNU devoted less time to rearing into open arms. In the HB task, MC mice displayed higher exploratory activity reflected in more head-dips (HD) during the first minute than EE and SE, whereas EE displayed low exploration levels reflected in total HD (5 min).
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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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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Bodnar AL, et al. J Med Chem. 2005 Feb 24, 48(4), 905-8.
2. Li F, et al. Shock. 2013 Feb, 39(2), 197-203.
3. Stuckenholz V, et al. J Parkinsons Dis. 2013, 3(2), 161-72.
4. Mesa-Gresa P, et al. Behav Processes. 2014 Mar, 103, 117-24.
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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SF9020-10mM
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PNU282987 (α7 nAChR激动剂)
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10mM×0.2ml
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SF9020-5mg
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PNU282987 (α7 nAChR激动剂)
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5mg
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SF9020-25mg
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PNU282987 (α7 nAChR激动剂)
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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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