Clozapine N-oxide dihydrochloride|2250025-93-3|(氯氮平N-氧化盐酸)-陌孚医药/Medlife

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Clozapine N-oxide dihydrochloride (Synonyms: 氯氮平N-氧化盐酸)

目录号: PL04704 纯度: ≥98%

CAS No. :2250025-93-3

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中文名称	Clozapine N-oxide dihydrochloride
中文别名	氯氮平N-氧化盐酸
英文名称	Clozapine N-oxide dihydrochloride
英文别名	Clozapine N-oxide (dihydrochloride);Clozapine N-oxide dihydrochloride
Cas No.	2250025-93-3
分子式	C₁₈H₂₁Cl₃N₄O
分子量	415.74
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情	Clozapine N-oxide dihydrochloride 是一种 Clozapine 的主要代谢产物，也是一种人毒蕈碱设计受体 (DREADDs) 激动剂。Clozapine N-oxide dihydrochloride 可激活 DREADD 受体 hM3Dq 和 hM4Di。Clozapine N-oxide dihydrochloride 可以穿过血脑屏障。Clozapine 是一种有效的多巴胺拮抗剂，也一种是有效的选择性毒蕈碱 M4 受体 (muscarinic M4 receptor) (EC₅₀ 为 11 nM) 激动剂。
生物活性	Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC 50 =11 nM) agonist.
性状	Solid
IC50 & Target[1][2]	Human muscarinic designer receptors (DREADDs)
体外研究(In Vitro)	Clozapine N-oxide (CNO) can bind to non-DREADD receptors at concentrations required for DREADD activation, and undergoes reverse-metabolism to its parent compound clozapine, an atypical antipsychotic that acts at a variety of pharmacological targets and produces numerous physiological and behavioral effects. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h). 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	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献	[1]. Wess J, et al. Novel designer receptors to probe GPCR signaling and physiology. Trends Pharmacol Sci. 2013 Jul;34(7):385-92. [2]. Manvich DF, et al. The DREADD agonist clozapine N-oxide (CNO) is reverse-metabolized to clozapine and produces clozapine-like interoceptive stimulus effects in rats and mice. Sci Rep. 2018 Mar 1;8(1):3840.

溶解度数据	In Vitro: DMSO : 240 mg/mL (577.28 mM; Need ultrasonic)H₂O : 100 mg/mL (240.53 mM; Need ultrasonic)配制储备液

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