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CLOZAPINE N-OXIDE

Catalog No. T4494 CAS 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.

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CLOZAPINE N-OXIDE, CAS 34233-69-7

Pack Size	Availability	Price/USD
2 mg	In stock	$ 30.00
5 mg	In stock	$ 45.00
10 mg	In stock	$ 76.00
25 mg	In stock	$ 126.00
50 mg	In stock	$ 187.00
100 mg	In stock	$ 278.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.94%

Purity: 99.84%

Purity: 99.72%

Purity: 99.66%

Purity: 99.6%

Purity: 99.47%

Purity: 98.65%

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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]

Molecular Weight	342.82
Formula	C18H19ClN4O
CAS No.	34233-69-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 1 mg/mL

Ethanol: 10 mg/mL

DMSO: 6 mg/mL, The compound is unstable in solution, please use soon.

References and Literature

1. Jendryka M, et al. Pharmacokinetic and pharmacodynamic actions of clozapine-N-oxide, clozapine, and compound 21 in DREADD-based chemogenetics in mice. Sci Rep. 2019 Mar 14;9(1):4522. 2. McDonough RC, et al. DREADD-based synthetic control of chondrocyte calcium signaling in vitro. J Orthop Res. 2019 Jul;37(7):1518-1529. 3. Traut J, et al. Effects of clozapine-N-oxide and compound 21 on sleep in laboratory mice. Elife. 2023 Mar 9;12:e84740. 4. Aomine Y, et al. Clozapine N-oxide, compound 21, and JHU37160 do not influence effortful reward-seeking behavior in mice. Psychopharmacology (Berl). 2024 Jan;241(1):89-96.

Citations

1. Ma X, Li L, Li Z, et al. eEF2 in the prefrontal cortex promotes excitatory synaptic transmission and social novelty behavior. EMBO reports. 2022: e54543. 2. Wang Y, Liu N, Ma L, et al.Ventral Hippocampal CA1 Pyramidal Neurons Encode Nociceptive Information.Neuroscience Bulletin.2023: 1-17.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Anti-Alzheimer's Disease Compound Library Angiogenesis related Compound Library Target-Focused Phenotypic Screening Library CNS-Penetrant Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Neurotransmitter Receptor Compound Library FDA-Approved & Pharmacopeia Drug Library Endocrinology-Hormone Compound Library

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Keywords

CLOZAPINE N-OXIDE 34233-69-7 GPCR/G Protein Metabolism Neuroscience Dopamine Receptor 5-HT Receptor Drug Metabolite AChR Clozapine N-oxide BBB DREADDs hM3Dq metabolite inhibit Inhibitor CLOZAPINE N OXIDE Clozapine G-protein Muscarinic acetylcholine receptor mAChR muscarinic-M4 CLOZAPINE NOXIDE inhibitor

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