产品编号 |
产品名称 |
产品包装 |
产品价格 |
SD2461-5mg |
Clozapine N-Oxide (5-HT2拮抗剂) |
5mg |
500.00元 |
化学信息:
化学名
|
3-chloro-6-(4-methyl-4-oxidopiperazin-4-ium-1-yl)-5H-benzo[b][1,4]benzodiazepine
|
|
简称
|
Clozapine N-Oxide
|
别名
|
Clozapine (N-oxide), N-Oxyclozapine
|
中文名
|
N/A
|
化学式
|
C18H19ClN4O
|
分子量
|
342.82
|
CAS号
|
34233-69-7
|
纯度
|
98%
|
溶剂/溶解度
|
Water35mg/ml; DMSO20mg/ml; Ethanol<1mg/ml
|
溶液配制
|
5mg加入1.46ml DMSO,或者每3.43mg加入1ml DMSO,配制成10mM溶液。SD2461-10mM用DMSO配制。
|
生物信息:
产品描述
|
Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.
|
信号通路
|
GPCR & G Protein; Neuronal Signaling
|
靶点
|
5-HT2
|
-
|
-
|
-
|
-
|
IC50
|
-
|
-
|
-
|
-
|
-
|
体外研究
|
Clozapine and N-desmethylclozapine antagonized 5-HT-stimulated phosphoinositide hydrolysis with IC50 values of 110 and 29.4nM, respectively. Clozapine N-oxide was less potent.
|
体内研究
|
When administered clozapine, mean CNO plasma concentrations of 17.7 +/- 16.4ng/ml were slightly lower than the other clozapine metabolite-desmethylclozapine (DCLOZ) plasma levels of 24.4 +/- 8.6ng/ml at the 12 hour time point. When CNO was administered, plasma concentrations at the 12 hour time point of clozapine were twice the amount of CNO (28.1 +/- 8.9ng/ml vs 14.4 +/- 8.8ng/ml). Clozapine and its metabolite clozapine-N-oxide (0.5mg/kg) were administered intraperitoneally to guinea-pigs. Significant amounts of clozapine were detected in plasma, liver, frontal cortex and caudate after clozapine-N-oxide administration.
|
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. Kuoppamki M, et al. Eur J Pharmacol. 1993 Apr 15, 245(2), 179-82.
2. Chang WH, et al. Prog Neuropsychopharmacol Biol Psychiatry. 1998 Jul, 22(5), 723-39.
3. Jann MW, et al. Arch Int Pharmacodyn Ther. 1994 Sep-Oct, 328(2), 243-50.
包装清单:
产品编号
|
产品名称
|
包装
|
SD2461-10mM
|
Clozapine N-Oxide (5-HT2拮抗剂)
|
10mM×0.2ml
|
SD2461-5mg
|
Clozapine N-Oxide (5-HT2拮抗剂)
|
5mg
|
SD2461-25mg
|
Clozapine N-Oxide (5-HT2拮抗剂)
|
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:
本产品对人体有害,操作时请小心,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。