Deschloroclozapine (Synonyms: 氯氮平杂质)
目录号: PL06892 纯度: ≥99%
CAS No. :1977-07-7
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中文名称
Deschloroclozapine
中文别名
11-(4-甲基-1-哌嗪基)-5H-二苯并[B,E][1,4]二氮杂卓;氯氮平杂质
英文名称
Deschloroclozapine
英文别名
5H-Dibenzo[b,e][1,4]diazepine,11-(4-methyl-1-piperazinyl)-;11-(4-METHYL-1-PIPERAZINYL)-5H-DIBENZO(B,E)(1,4)DIAZEPINE;Dopamine serotonin antagonist-1;11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine;5H-Dibenzo(b,e)(1,4)diazepine, 11-(4-methyl-1-piperazinyl)-;BRN 0761696;11-(4-Methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine;11-(4-Methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine;VQHITFFJBFOMBG-UHFFFAOYSA-N;BDBM50010591;Deschloroclozapine
Cas No.
1977-07-7
分子式
C18H20N4
分子量
292.38
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
Deschloroclozapine 是氯氮平的代谢物,是一种高效的毒蕈碱 DREADDs 激动剂。Deschloroclozapine 对 DREADD 受体亚型 hM3Dq 和 hM4Di 结合 Ki 值分别为 6.3 和 4.2 nM。[11C]-Deschloroclozapine 是一种有前途的 PET 示踪剂,可用于 DREADD 的影像学检查。
生物活性
Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with K i of 6.3 and 4.2 nM, respectively. [C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging.
性状
Solid
IC50 & Target[1][2]
Ki: 6.3 nM (hM3Dq), 4.2 nM (hM4Di)
体外研究(In Vitro)
Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a chemogenetic approach for remote manipulation of neuronal activity in freely-moving animals. DREADDs comprise mutated G protein-coupled receptors (GPCRs) that do not respond to their endogenous neurotransmitter, but do respond to an otherwise “inert” exogenous substance. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Deschloroclozapine (0.3?mg/kg; intramuscularly) impairs working memory function in male rhesus macaques (aged between 5 and 6 years and weighing 5.5-7.9?kg).
Deschloroclozapine (0.1?mg/kg; i.m) is effective at activating DREADD receptors in vivo and reversibly inducing behavioral effects in monkeys. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Maggs JL, et al. The metabolic formation of reactive intermediates from clozapine, a drug associated with agranulocytosis in man. J Pharmacol Exp Ther. 1995;275(3):1463-1475.
[2]. Hu F, et al. F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography. Eur J Med Chem. 2021;213:113047.
溶解度数据
In Vitro: DMSO : 100 mg/mL (342.02 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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