| 产品编号 |
产品名称 |
产品包装 |
产品价格 |
| SD9563-10mM |
Brexpiprazole (Dopamine Receptor激动剂) |
10mM |
108.00元 |
化学信息：
|
化学名
|
7-[4-[4-(1-benzothiophen-4-yl)piperazin-1-yl]butoxy]-1H-quinolin-2-one
|
|
|
简称
|
Brexpiprazole
|
|
别名
|
OPC-34712, Rexulti, GTPL7672
|
|
中文名
|
依匹唑派
|
|
化学式
|
C25H27N3O2S
|
|
分子量
|
433.57
|
|
CAS号
|
913611-97-9
|
|
纯度
|
98%
|
|
溶剂/溶解度
|
Water<1mg/ml; DMSO24mg/ml; Ethanol<1mg/ml
|
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溶液配制
|
5mg加入1.15ml DMSO，或者每4.34mg加入1ml DMSO，配制成10mM溶液。SD9563-10mM用DMSO配制。
|
生物信息：
|
产品描述
|
Brexpiprazole is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors.
|
|
信号通路
|
Neuronal Signaling; GPCR & G Protein
|
|
靶点
|
5-HT1A
|
human noradrenergic α1B
|
Dopamine D2L
|
5-HT2A receptors
|
α2C receptors
|
|
IC50
|
0.12nM(Ki)
|
0.17nM(Ki)
|
0.3nM(Ki)
|
0.47nM(Ki)
|
0.59nM(Ki)
|
|
体外研究
|
Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12nM) and dopamine D2L (Ki=0.3nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17nM) and α2Creceptors (Ki=0.59nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiatedngF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth.
|
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体内研究
|
Brexpiprazole is able to ameliorate PCP-191 induced cognitive deficits in mice, via 5-HT1A receptors.
|
|
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
|
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细胞实验
|
|
细胞系
|
PC12 cells
|
|
浓度
|
0.001，0.01，0.1或1.0μM
|
|
处理时间
|
4 days
|
|
方法
|
2.5ng/ml of ngF (nerve growth factor) is used to study the potentiating effects of brexpiprazole on neurite outgrowth. Twenty-four hours after plating, the medium is replaced with DMEM medium containing 0.5% FBS and 1% penicillin-streptomycin withngF (2.5ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0μM). Four days after incubation withngF (2.5ng/ml) with or without drugs, morphometric analysis is performed on digitized images of live cells taken under phase-contrast illumination, with an inverted microscope linked to a camera.
|
|
动物实验
|
|
动物模型
|
Male ICR mice
|
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配制
|
0.5% methylcellulose
|
|
剂量
|
0.3, 1, or 3mg/kg/day
|
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给药方式
|
oral administration
|
参考文献：
1. Ishima T, et al. Eur Neuropsychopharmacol. 2015, 25(4):505-511.
2. Yoshimi N, et al. Pharmacol Biochem Behav. 2014, 124:245-249.
包装清单：
|
产品编号
|
产品名称
|
包装
|
|
SD9563-10mM
|
Brexpiprazole (Dopamine Receptor激动剂)
|
10mM×0.2ml
|
|
SD9563-5mg
|
Brexpiprazole (Dopamine Receptor激动剂)
|
5mg
|
|
SD9563-25mg
|
Brexpiprazole (Dopamine Receptor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。
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。