CAS 34233-69-7; e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo( n-oxide

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CAS:

34233-69-7

分子式:

C18H19ClN4O

分子量:

342.82

英文名称:

e)(1,4)diazepine, 8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo( n-oxide

8-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine n-oxide

clozapine n-oxide

vufb-12426

用途:

Clozapine (N-oxide)，Clozapine 在药理学上的惰性代谢物，是一种抗精神病药。Clozapine (N-oxide) 是 DREADD 系统的激动剂。Clozapine 是多巴胺和许多其他受体的有效拮抗剂。Clozapine 也是选择性的毒蕈碱 M4 受体的激动剂 (EC50=11 nM)。

推荐供应商

货号

品牌

产品名称

规格

包装、参考价格

C879476

MACKLIN

Clozapine (N-oxide)

≥99%

116元/1mg; 322元/5mg; 495元/10mg; 1499元/50mg; 5398元/250mg; 13500元/1g;

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储存：2-8℃
状态：浅黄色到黄色固体

C766704

MACKLIN

Clozapine (N-oxide)

10mM in DMSO

669元/1ml;

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储存：-20°C

C0832

Sigma-Aldrich

Clozapine N-oxide

2782.13元/5 MG;

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产品说明

一般描述

氯氮平N-氧化物(CNO)，氯氮平药物的非激活形式，可活化G蛋白偶联受体(GPCR)。CNO看作为工程化人毒蕈碱受体的合成配体。它在代谢转化时可引起类似氯氮平的作用。氯氮平转化为CNO将有利于其通过血脑屏障。

应用

氯氮平N-氧化物已用于：

在初级运动皮层中激活人M4毒蕈碱(hM4Di)
在Th-cre转基因小鼠中诱导体内化学遗传性操控并损伤运动活性
小鼠中的行为测试和刺激(HEK293)细胞

包装

5 mg in glass bottle

生化/生理作用

5-HT₂血清素受体拮抗剂；可通过HPLC监测的氯吡啶主要代谢产物。

特点和优势

该化合物是神经科学研究的特色产品。点击此处以了解更多的神经科学特色产品。可访问sigma.com/discover-bsm了解更多关于用于其他研究领域生物活性小分子。

基本信息

经验(实验)分子式	C₁₈H₁₉ClN₄O
分子量	342.82
MDL编号	MFCD00210190
PubChem化学物质编号	24892276
NACRES	NA.77

产品性质

质量水平	200
SMILES string	C[N+]1([O-])CCN(CC1)C2=Nc3cc(Cl)ccc3Nc4ccccc24
InChI	1S/C18H19ClN4O/c1-23(24)10-8-22(9-11-23)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
InChI key	OGUCZBIQSYYWEF-UHFFFAOYSA-N

安全信息

象形图
警示用语：	Danger
危险声明	H301 - H336
预防措施声明	P301 + P310 + P330
危险分类	Acute Tox. 3 Oral - STOT SE 3
靶器官	Central nervous system
储存分类代码	6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable
个人防护装备	dust mask type N95 (US), Eyeshields, Faceshields, Gloves

SML2304

Sigma-Aldrich

Clozapine N-oxide hydrochloride

≥98% (HPLC), Water soluble Clozapine N-oxide

2255.27元/5 MG;

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产品说明

一般描述

Clozapine N-oxide hydrochloride is a water soluble form of Clozapine N-oxide (CNO) (Sigma cat# C0832). CNO is a pharmacologically inert metabolite of the atypical anti-psychotic drug clozapine. CNO is a ligand for the engineered Gq protein coupled receptors (GPCRs) in the chemogenetic Designer Receptors Exclusively Activated by Designer Drug (DREADD). The typical use of DREADD is testing, enhancing neuronal firing and activating Gq signaling in neuronal and non-neuronal cells.
The selective targeting of DREADD systems to cell population can be achieved by using a cell type-specific promoter to drive DREADD expression, and the expression of this promoter can be further controlled using a recombinase-based system. DREADDs possess a low affinity for endogenous ligands and little constitutive activity, but may be activated by synthetic compounds such as CNO.
DREADD systems are activated by low nM concentrations of CNO and mobilize intracellular calcium. CNO appears to be pharmacologically and behaviorally inert in mice and rats when administered at the recommended doses (generally 0.1–3 mg/kg). CNO is commonly administrated via injection but also can be mixed into food chow or drinking water.

其他说明

High concentration Solutions of (40mg/ml) can be prepared from the water soluble CNO and be used in CNO applications without the use of DMSO.

基本信息

经验(实验)分子式	C₁₈H₁₉ClN₄O · xHCl
分子量	342.82 (free base basis)
NACRES	NA.77

产品性质

生物来源	synthetic
测定	≥98% (HPLC)
形式	powder
储存条件	desiccated
溶解性	DMSO: 40 mg/mL water: 40 mg/mL
运输	ambient
储存温度	2-8℃
SMILES string	ClC1=CC2=C(NC(C=CC=C3)=C3C(N4CC[N+]([O-])(C)CC4)=N2)C=C1.[xHCl]

安全信息

象形图
警示用语：	Danger
危险声明	H301 - H336
预防措施声明	P301 + P310 + P330
危险分类	Acute Tox. 3 Oral - STOT SE 3
靶器官	Central nervous system
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

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