Deschloroclozapine

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Cat.No. 7193 - Deschloroclozapine | C18H20N4 | CAS No. 1977-07-7
Description: High affinity and highly potent activator of hM3Dq and hM4Di DREADDs; rapidly blood brain barrier penetrant
Alternative Names: DCZ
Chemical Name: 11-(4-Methyl-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

High affinity and highly potent activator of muscarinic DREADDs (Ki values are 6.3 nM for hM3Dq and 4.2 nM for hM4Di, in vitro; EC50 values are 0.13 nM for hM3Dq and 0.081 nM for hM4Di, in vitro). Derivative of clozapine (Cat. No. 0444). Exhibits 100-fold greater affinity for hM3Dq and hM4Di compared to clozapine N-oxide (CNO; Cat. No. 4936), and 50-fold greater affinity compared to DREADD agonist 21 (Cat. No. 5548). Displays low 'off-target' receptor binding (Ki >100 nM at majority of GPCRs, ion channels and transporters tested). Displays rapid (approx. 10 minutes after i.p injection) binding and activation of hM3Dq and hM4Di in mice and non-human primates. Induces spatial memory deficits in non-human primates expressing hM4Di in the prefrontal cortex.

Technical Data

M. Wt 292.39
Formula C18H20N4
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1977-07-7
PubChem ID 16103
InChI Key VQHITFFJBFOMBG-UHFFFAOYSA-N
Smiles CN1CCN(C2=NC3=C(C=CC=C3)NC4=CC=CC=C24)CC1

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
DMSO 29.24 100
ethanol 29.24 100

Preparing Stock Solutions

The following data is based on the product molecular weight 292.39. 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
1 mM 3.42 mL 17.1 mL 34.2 mL
5 mM 0.68 mL 3.42 mL 6.84 mL
10 mM 0.34 mL 1.71 mL 3.42 mL
50 mM 0.07 mL 0.34 mL 0.68 mL

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References

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

Nagai et al (2020) Deschloroclozapine, a potent and selective chemogenetic actuator enables rapid neuronal and behavioral modulations in mice and monkeys Nat.Neurosci. 23 1157 PMID: 32632286


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Keywords: Deschloroclozapine, Deschloroclozapine supplier, clozapine, metabolite, clozapine-N-oxide, DREADDs, DREADD, Ligands, muscarnic, receptors, designer, CNO, chemogenetics, DCZ, potent, BBB, brain, blood, barrier, penetrant, Non-selective, Muscarinics, 7193, Tocris Bioscience

Citations for Deschloroclozapine

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Literature in this Area

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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.

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