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Clozapine N-Oxide

Name: Clozapine N-Oxide
Brand: TargetMol
SKU: T4494
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4494Cas No. 34233-69-7

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Clozapine N-Oxide

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Purity: 99.94%

Catalog No. T4494Cas No. 34233-69-7

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	In Stock	In Stock
5 mg	$45	In Stock	In Stock
10 mg	$76	In Stock	In Stock
25 mg	$126	In Stock	In Stock
50 mg	$187	In Stock	In Stock
100 mg	$278	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.94%

Color:White to Yellow

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COA

Product Introduction

Bioactivity

Description	Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.
Targets&IC50	M4Di (human):8.1 nM (EC50), CYP2B6:8.3 µM, CYP2C19:8.7 µM
In vitro	METHODS: hM4Di-transduced primary embryonic rat neuronal cultures were treated with Clozapine N-oxide (0.01-1000 nM), and activity on hM4Di receptors was detected by FLIPR assay. RESULTS: The EC50 value for Clozapine N-oxide was 8.1 nM. [1] METHODS: WT and hM3Dq-transfected mouse embryoma cells ATDC5 were treated with Clozapine N-oxide (750 nM) to detect intracellular calcium signaling. RESULTS: Administration of Clozapine N-oxide resulted in immediate coordinated induction of single [Ca2+]i spines in hM3Dq-ATDC5 cells, and only spontaneous [Ca2+]i signaling was observed in Clozapine N-oxide-treated WT controls. [2]
In vivo	METHODS: To investigate potential effects on sleep, Clozapine N-oxide (1-10 mg/kg) was injected intraperitoneally into C57BL/6J mice. RESULTS: Clozapine N-oxide altered sleep in mice. Sleep was analyzed using electroencephalography (EEG) and electromyography (EMG), revealing dose-dependent suppression of rapid eye movement (REM) sleep, changes in EEG spectral power during non-rapid eye movement (NREM) sleep, and alterations in sleep structure. [3] METHODS: To investigate the effects on reward-seeking behavior, Clozapine N-oxide (0.1-10 mg/kg) was administered intraperitoneally to C57BL6/JJcl mice. RESULTS: The off-target effects of commonly used doses of Clozapine N-oxide on motivated reward seeking were negligible. [4]

Chemical Properties

Molecular Weight	342.82
Formula	C₁₈H₁₉ClN₄O
Cas No.	34233-69-7
Smiles	CN1(=O)CCN(C=2C=3C(NC=4C(N2)=CC(Cl)=CC4)=CC=CC3)CC1
Relative Density.	1.36g/cm3

Storage & Solubility Information

Storage

The compound is unstable in solution. Please use soon | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 1 mg/mL (2.92 mM), Sonication is recommended. The compound is unstable in solution, please use soon.

Ethanol: 10 mg/mL (29.17 mM), Sonication is recommended. The compound is unstable in solution, please use soon.

DMSO: 252.5 mg/mL (736.54 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (9.63 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9170 mL	14.5849 mL	29.1698 mL	145.8491 mL

Ethanol/DMSO

	1mg	5mg	10mg	50mg
5 mM	0.5834 mL	2.9170 mL	5.8340 mL	29.1698 mL
10 mM	0.2917 mL	1.4585 mL	2.9170 mL	14.5849 mL
20 mM	0.1458 mL	0.7292 mL	1.4585 mL	7.2925 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0583 mL	0.2917 mL	0.5834 mL	2.9170 mL
100 mM	0.0292 mL	0.1458 mL	0.2917 mL	1.4585 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc