Clozapine N-oxide

Name: Clozapine N -oxide
Brand: Tocris Bioscience
SKU: 4936
Rating: 5 (2 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4936

(2)

Citations (390)

COA / SDS

Activator of hM3Dq and hM4Di DREADDs

Key Product Details

Description:	Activator of hM₃D_q and hM₄D_i DREADDs
Alternative Names:	CNO
Chemical Name:	8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity:	≥99% (HPLC)
Molecular Weight:	342.82

View Full Technical Details for Clozapine N-oxide

Technical Data
Citations / Reviews (2)

Biological Activity for Clozapine N-oxide

Clozapine N-oxide is a synthetic ligand for human muscarinic engineered receptors, designer receptors activated by designer drugs (DREADD). Binds and activates hM₃D_q and hM₄D_i DREADDs in vitro and in vivo. Metabolite of Clozapine (Cat. No. 0444). Shown to be a P-glycoprotein (P-gp) efflux pump substrate.

Example Applications of Clozapine N-oxide (CNO):

Silences hippocampal neurons expressing hM₄D_i DREADDs in vitro
Inhibits locomotor activity of mice expressing hM₃D_q in GABAergic VTA neurons
Inhibits short term memory retrieval in mice expressing hM₄D_i in hippocampal neurons
Induces heat and mechanical hypersensitivity in mice expressing hM₄D_i in enkephalinergic neurons in the right lumbar dorsal horn
Inhibits markers of social aggression in mice expressing hM₄D_i in hippocampal CA2 neurons

Alternative potent and selective hM₃D_q and hM₄D_i DREADD agonists available: Deschloroclozapine and DREADD agonist 21

Water soluble salt also available.

This product contains 1 molar equivalent of ethanol.

Technical Data for Clozapine N-oxide

M. Wt	342.82
Formula	C₁₈H₁₉ClN₄O
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	34233-69-7
PubChem ID	2819
InChi Key	WYRDWWAASBTJLM-UHFFFAOYSA-N
Smiles	ClC(C=C3)=CC1=C3NC(C=CC=C2)=C2C(N4CC[N+](C)([O-])CC4)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Clozapine N-oxide

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	6.86	20

Preparing Stock Solutions for Clozapine N-oxide

The following data is based on the product molecular weight 342.82.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	14.58 mL	72.92 mL	145.85 mL
1 mM	2.92 mL	14.58 mL	29.17 mL
2 mM	1.46 mL	7.29 mL	14.58 mL
10 mM	0.29 mL	1.46 mL	2.92 mL

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References for Clozapine N-oxide

References are publications that support the biological activity of the product.

Roth DREADDs for Neuroscientists. Neuron 2016 PMID: 26889809
Nakajima G_s-coupled GPCR signalling in AgRP neurons triggers sustained increase in food intake. Nat.Commun. 2016 PMID: 26743492
Gomez Chemogenetics revealed: DREADD occupancy and activation via converted cloz. Science 2017 PMID: 28774929
Zaman LMO4 is essential for paraventricular hypothalamic neuronal activity and calcium channel expression to prevent hyperphagia. J.Neurosci. 2014 PMID: 24381275
Armbruster Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand. Proc.Natl.Acad.Sci.U.S.A. 2007 PMID: 17360345
Eiermann The involvement of CYP1A2 and CYP3A4 in the metabolism of cloz. Br.J.Clin.Pharmacol. 1997 PMID: 9384460