Clozapine N-oxide dihydrochloride

Pricing Availability   Qty
Cat.No. 6329 - Clozapine N-oxide dihydrochloride | C18H19ClN4O.2HCl | CAS No. 2250025-93-3
Description: Activator of muscarinic DREADDs; water soluble version of Clozapine N-oxide (Cat. No. 4936)
Chemical Name: 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews (1)
Literature (4)

Biological Activity

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

Technical Data

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 Data

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

Preparing Stock Solutions

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 1.2 mL 2.41 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:

References

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

Eiermann et al (1997) The involvement of CYP1A2 and CYP3A4 in the metabolism of cloz. Br.J.Clin.Pharmacol. 44 439 PMID: 9384460

Ambruster et al (2007) 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. 104 5163 PMID: 17360345

Zaman et al (2014) LMO4 is essential for paraventricular hypothalamic neuronal activity and calcium channel expression to prevent hyperphagia. J.Neurosci. 34 140 PMID: 24381275

Gomez et al (2017) Chemogenetics revealed: DREADD occupancy and activation via converted cloz. Science 357 503 PMID: 28774929

Roth et al (2016) DREADDs for Neuroscientists. Neuron 89 683 PMID: 26889809

Nakajima et al (2016) Gs-coupled GPCR signalling in AgRP neurons triggers sustained increase in food intake. Nat.Commun. 8 10268 PMID: 26743492

Allen et al (2019) A comparative study of the pharmacokinetics of cloz. N-oxide and cloz. N-oxide hydrochloride salt in rhesus macaques. J.Pharmacol.Exp.Ther. 368 199 PMID: 30523062


If you know of a relevant reference for Clozapine N-oxide dihydrochloride, please let us know.

Keywords: Clozapine N-oxide dihydrochloride, Clozapine N-oxide dihydrochloride supplier, Clozapine, N-oxide, 2HCl, metabolite, 5HT2A/2C, non-selective, serotonin, 5HT2C, 5HT2, 5HT2A, dopaminergic, dopamine, antagonists, D4, DREADDs, Ligands, muscarnic, designer, receptors, CNO, water, soluble, Multidrug, Transporters, Non-selective, Muscarinics, 6329, Tocris Bioscience

4 Citations for Clozapine N-oxide dihydrochloride

Citations are publications that use Tocris products. Selected citations for Clozapine N-oxide dihydrochloride include:

Chang et al (2019) The Ventral Hippocampus Controls Stress-Provoked Impulsive Aggression through the Ventromedial Hypothalamus in Post-Weaning Social Isolation Mice. Cell Rep 28 1195 PMID: 31365864

Torre-Muruzabal et al (2019) Chronic nigral neuromodulation aggravates behavioral deficits and synaptic changes in an a-synuclein based rat model for Parkinson's disease. Acta Neuropathol Commun 7 160 PMID: 31640762

Khodai et al (2018) PACAP Neurons in the Ventromedial Hypothalamic Nucleus Are Glucose Inhibited and Their Selective Activation Induces Hyperglycaemia. Front Endocrinol (Lausanne) 9 632 PMID: 30425681

Fernandez et al (2018) Thalamic reticular control of local sleep in mouse sensory cortex. Elife 7 PMID: 30583750


Do you know of a great paper that uses Clozapine N-oxide dihydrochloride from Tocris? Please let us know.

Reviews for Clozapine N-oxide dihydrochloride

Average Rating: 5 (Based on 1 Review.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%

Have you used Clozapine N-oxide dihydrochloride?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:


Great H2O soluble version of CNO.
By Melanie Pina on 05/23/2019
Assay Type: In Vivo
Species: Mouse

Great water soluble version that worked beautifully in my hands. Used to stimulate virally-expressed hM4Di for behavioral neuroscience applications. CNO-induced activation of hM4Di significantly inhibited neuronal activation as confirmed via c-Fos staining.

review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Chemogenetics

Chemogenetics Research Bulletin

Produced by Tocris, the chemogenetics research bulletin provides an introduction to chemogenetic methods to manipulate neuronal activity. It outlines the development of RASSLs, DREADDs and PSAMs, and the use of chemogenetic compounds. DREADD ligands and PSEMs available from Tocris are highlighted.

Allosteric GPCR Pharmacology

Allosteric GPCR Pharmacology Poster

G protein-coupled receptors (GPCRs) are intrinsically allosteric proteins. This poster provides insights into allosteric mechanisms of GPCR biology, highlighting key facets of GPCR allostery and therapeutic applications of allosteric modulators.

GPCR Efficacy and Biased Agonism

GPCR Efficacy and Biased Agonism Poster

GPCRs can interact with multiple distinct transducers or regulatory proteins and these can be preferentially engaged in an agonist-specific manner giving rise to biased agonism. This poster discusses cutting edge GPCR signaling pharmacology and highlights therapeutic applications of biased agonism.