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 |
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。