Clozapine N-oxide dihydrochloride

Name: Clozapine N-oxide dihydrochloride
Brand: MedChemExpress
SKU: HY-17366A
Rating: 5.0 (145 reviews)

製品番号: HY-17366A 純度: 99.74%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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 cannot cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 2250025-93-3

容量	価格（税別）	在庫状況	数量
>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
5 mg	$58	在庫あり	Estimated Time of Arrival: December 31
10 mg	$95	在庫あり	Estimated Time of Arrival: December 31
25 mg	$200	在庫あり	Estimated Time of Arrival: December 31
50 mg	$320	在庫あり	Estimated Time of Arrival: December 31
100 mg	$520	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 145 publication(s) in Google Scholar

Other Forms of Clozapine N-oxide dihydrochloride:

Clozapine N-oxide 在庫あり
Clozapine N-oxide dihydrochloride (Standard) お問い合わせ

顧客検証

In Vivo Efficacy Study

: Clozapine N-oxide dihydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May;12(18):e2412822. [Abstract]; Examples of respiratory waveforms in mice after injection of saline and CNO (1 mg/kg, i.p.) respectively.

: Clozapine N-oxide dihydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May;12(18):e2412822. [Abstract]; The injection (1 mg/kg, i.p.) of CNO produced a long‐lasting decrease in BF and MV rather than TV in Vgat‐Cre mice (n = 15 for each group). All error bars show mean ± s.e.m.

: Clozapine N-oxide dihydrochloride purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2025 Oct 2;22(1):222. [Abstract]; Statistical analysis of calcium transients in sham-operated mice after intraventricular injection of LPS followed by intraperitoneal injection of CNO (5 mg/kg) or saline.

: Clozapine N-oxide dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Oct 5;15(1):8632. [Abstract]; Compared with the control group expressing AAV-DIO-mCherry in CRH neurons, intraperitoneal injection of CNO (1 mg/kg bodyweight in saline, i.p.) in mice increased blood glucose levels.

: Clozapine N-oxide dihydrochloride purchased from MedChemExpress. Usage Cited in: Biol Psychiatry. 2017 May 1;81(9):737-747. [Abstract]; c-fos immunoreactivity in the VTA 90 minutes after injections of 1 mg/kg Clozapine N-oxide (CNO).

mAChR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

Dopamine Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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 cannot cross the blood-brain barrier^[1]^[2]^[3]^[4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist^[5]^[6].

IC₅₀ & Target

mAChR3

mAChR4

体外実験

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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

415.74

分子式

C₁₈H₂₁Cl₃N₄O

CAS 番号

2250025-93-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

C[N+]1([O-])CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC=C42)CC1.[H]Cl.[H]Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶剤 & 溶解度

体外:

DMSO : ≥ 200 mg/mL (481.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (240.53 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4053 mL	12.0267 mL	24.0535 mL
5 mM	0.4811 mL	2.4053 mL	4.8107 mL
10 mM	0.2405 mL	1.2027 mL	2.4053 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 20 mg/mL (48.11 mM); Clear solution

This protocol yields a clear solution of ≥ 20 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (200.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 20 mg/mL (48.11 mM); Clear solution

This protocol yields a clear solution of ≥ 20 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (200.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 20 mg/mL (48.11 mM); Clear solution

This protocol yields a clear solution of ≥ 20 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (200.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Saline
Solubility: 100 mg/mL (240.53 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.74%

Select Batch:

データシート (279 KB) SDS (420 KB)

COA (253 KB) HNMR (142 KB) RP-HPLC (247 KB) LCMS (101 KB)

取扱説明書 (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. van der Peet PL, et al. Gram scale preparation of clozapine N-oxide (CNO), a synthetic small molecule actuator for muscarinic acetylcholine DREADDs. MethodsX. 2018 Mar 23;5:257-267. [Content Brief]

[4]. Joseph Cichon, et al. Branch-specific dendritic Ca(2+) spikes cause persistent synaptic plasticity. Nature. 2015 Apr 9;520(7546):180-5. [Content Brief]

[5]. Silva RR, et al. Evaluation of Functional Selectivity of Haloperidol, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine D2 Receptor. Front Pharmacol. 2019 Jun 4;10:628. [Content Brief]

[6]. Zorn SH, et al. Clozapine is a potent and selective muscarinic M4 receptor agonist. Eur J Pharmacol. 1994 Nov 15;269(3):R1-2. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.4053 mL	12.0267 mL	24.0535 mL	60.1337 mL
	5 mM	0.4811 mL	2.4053 mL	4.8107 mL	12.0267 mL
	10 mM	0.2405 mL	1.2027 mL	2.4053 mL	6.0134 mL
	15 mM	0.1604 mL	0.8018 mL	1.6036 mL	4.0089 mL
	20 mM	0.1203 mL	0.6013 mL	1.2027 mL	3.0067 mL
	25 mM	0.0962 mL	0.4811 mL	0.9621 mL	2.4053 mL
	30 mM	0.0802 mL	0.4009 mL	0.8018 mL	2.0045 mL
	40 mM	0.0601 mL	0.3007 mL	0.6013 mL	1.5033 mL
	50 mM	0.0481 mL	0.2405 mL	0.4811 mL	1.2027 mL
	60 mM	0.0401 mL	0.2004 mL	0.4009 mL	1.0022 mL
	80 mM	0.0301 mL	0.1503 mL	0.3007 mL	0.7517 mL
	100 mM	0.0241 mL	0.1203 mL	0.2405 mL	0.6013 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.