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Clozapine N-Oxide

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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

Clozapine N-Oxide

🥰Excellent
Purity: 99.94%
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.
Pack SizePriceAvailabilityQuantity
2 mg$30In Stock
5 mg$45In Stock
10 mg$76In Stock
25 mg$126In Stock
50 mg$187In Stock
100 mg$278In Stock
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Purity:99.94%
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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.
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 Weight342.82
FormulaC18H19ClN4O
Cas No.34233-69-7
SmilesCN1(=O)CCN(C=2C=3C(NC=4C(N2)=CC(Cl)=CC4)=CC=CC3)CC1
Relative Density.1.36g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | Shipping with blue ice.
Solubility Information
Saline: 25 mg/mL (72.92 mM)
H2O: 1 mg/mL (2.92 mM), Sonication is recommended.
Ethanol: 10 mg/mL
DMSO: 60 mg/mL (175.02 mM), The compound is unstable in solution, please use soon.
Solution Preparation Table
H2O/Saline/DMSO
1mg5mg10mg50mg
1 mM2.9170 mL14.5849 mL29.1698 mL145.8491 mL
Saline/DMSO
1mg5mg10mg50mg
5 mM0.5834 mL2.9170 mL5.8340 mL29.1698 mL
10 mM0.2917 mL1.4585 mL2.9170 mL14.5849 mL
20 mM0.1458 mL0.7292 mL1.4585 mL7.2925 mL
50 mM0.0583 mL0.2917 mL0.5834 mL2.9170 mL
DMSO
1mg5mg10mg50mg
100 mM0.0292 mL0.1458 mL0.2917 mL1.4585 mL

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