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Submit ReviewDeschloroclozapine
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)
Biological Activity for Deschloroclozapine
Deschloroclozapine is a 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 for Deschloroclozapine
| 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 for Deschloroclozapine
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 29.24 | 100 | |
| ethanol | 29.24 | 100 |
Preparing Stock Solutions for Deschloroclozapine
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.
| 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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Product Datasheets for Deschloroclozapine
References for Deschloroclozapine
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
If you know of a relevant reference for Deschloroclozapine, please let us know.
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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
1 Citation for Deschloroclozapine
Citations are publications that use Tocris products. Selected citations for Deschloroclozapine include:
David E et al (2022) A serotonergic axon-cilium synapse drives nuclear signaling to alter chromatin accessibility. Cell 185 3390-3407.e18 PMID: 36055200
Do you know of a great paper that uses Deschloroclozapine from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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 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 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.