Clozapine N-oxide dihydrochloride

Name: Clozapine N -oxide dihydrochloride
Brand: Tocris Bioscience
SKU: 6329
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 6329

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Citations (61)

COA / SDS

Activator of hM3Dq and hM4Di DREADDs; water soluble version of Clozapine N-oxide (Cat. No. 4936)

Key Product Details

Description:	Activator of hM₃D_q and hM₄D_i DREADDs; water soluble version of Clozapine N-oxide (Cat. No. 4936)
Alternative Names:	CNO (water-soluble)
Chemical Name:	8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	415.74

View Full Technical Details for Clozapine N-oxide dihydrochloride

Technical Data
Citations / Reviews (1)

Biological Activity for Clozapine N-oxide dihydrochloride

Clozapine N-oxide dihydrochloride is a water-soluble salt of Clozapine N-oxide (Cat. No.4936). Activator of muscarinic DREADDs. Clozapine N-oxide dihydrochloride exhibits improved bioavailability (6 - 7-fold higher plasma concentration) compared with CNO, with less conversion to clozapine in animal studies.

Compound Libraries for Clozapine N-oxide dihydrochloride

Clozapine N-oxide dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Clozapine N-oxide dihydrochloride

M. Wt	415.74
Formula	C₁₈H₁₉ClN₄O.2HCl
Storage	Desiccate at RT
Purity	≥99% (HPLC)
CAS Number	2250025-93-3
PubChem ID	137187247
InChi Key	MBRGKRXDVKTUPT-UHFFFAOYSA-N
Smiles	ClC(C=C1)=CC2=C1NC(C=CC=C3)=C3C(N4CC[N+](C)([O-])CC4)=N2.Cl.Cl

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 dihydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	41.57	100
	DMSO	41.57	100

Preparing Stock Solutions for Clozapine N-oxide dihydrochloride

The following data is based on the product molecular weight 415.74.

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.41 mL	12.03 mL	24.05 mL
5 mM	0.48 mL	2.41 mL	4.81 mL
10 mM	0.24 mL	1.20 mL	2.41 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

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References for Clozapine N-oxide dihydrochloride

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

Nakajima G_s-coupled GPCR signalling in AgRP neurons triggers sustained increase in food intake. Nat.Commun. 2016 PMID: 26743492
Allen A comparative study of the pharmacokinetics of cloz. N-oxide and cloz. N-oxide hydrochloride salt in rhesus macaques. J.Pharmacol.Exp.Ther. 2019 PMID: 30523062
Roth DREADDs for Neuroscientists. Neuron 2016 PMID: 26889809
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
Ambruster 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