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
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.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。
象形图 |
|
警示语 |
|
Class |
|
警告声明 |
|
UNub |
|
危险声明 |
|
Packing Group |
|
暂无说明书!