Clozapine N-oxide

Pricing Availability Delivery Time Qty
Cat.No. 4936 - Clozapine N-oxide | C18H19ClN4O | CAS No. 34233-69-7
Description: Activator of muscarinic DREADDs
Chemical Name: 8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Literature

Biological Activity

Metabolite of clozapine (Cat. No. 0444). Activates human muscarinic designer receptors (DREADDs) in vitro. Silences hippocampal neurons expressing hM4 DREADDs in vitro. Activates Gs-linked DREADDS- AgRP in mice via intracerebroventricular (i.c.v) injection. Shown to be a P-glycoprotein (P-gp) efflux pump substrate. Other potent and selective hM3Dq DREADD agonists available: DREADD agonist 21 (Cat. No. 5548) and Perlapine (Cat. No. 5549)

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.86 20
ethanol 3.43 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 342.82. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 2.92 mL 14.58 mL 29.17 mL
5 mM 0.58 mL 2.92 mL 5.83 mL
10 mM 0.29 mL 1.46 mL 2.92 mL
50 mM 0.06 mL 0.29 mL 0.58 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

Armbruster 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 clozapine. Science 357 503 PMID: 28774929

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

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


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

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2 Citations for Clozapine N-oxide

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

D'Agostino et al (2016) Appetite controlled by a cholecystokinin nucleus of the solitary tract to hypothalamus neurocircuit. PLoS Biol 5 PMID: 26974347

Pina and Cunningham et al (2016) Ethanol-seeking behavior is expressed directly through an extended amygdala to midbrain neural circuit Neurobiology of Learning and Memory 137 83 PMID: 27866960


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