化学信息：
| 化学名 | N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-4-chlorobenzamide |
|
| 简称 | PNU282987 | |
| 别名 |
PNU 282987, PNU-282987 |
|
| 中文名 | N/A | |
| 化学式 | C14H18Cl2N2O | |
| 分子量 | 301.21 | |
| CAS号 | 123464-89-1 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO61mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 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。 |
生物信息：
| 产品描述 | 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). | ||||
| 信号通路 | Transmembrane Transporters; Neuronal Signaling | ||||
| 靶点 | α7 nAChR agonist | － | － | － | － |
| IC50 | 26nM(Ki) | － | － | － | － |
| 体外研究 | 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. | ||||
| 体内研究 | 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). | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
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)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SF9020-10mM | PNU282987 (α7 nAChR激动剂) | 10mM×0.2ml |
| SF9020-5mg | PNU282987 (α7 nAChR激动剂) | 5mg |
| SF9020-25mg | PNU282987 (α7 nAChR激动剂) | 25mg |
| — | 说明书 | 1份 |
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。
