DREADD agonist 21

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Cat.No. 5548 - DREADD agonist 21 | C17H18N4 | CAS No. 56296-18-5
Description: Potent muscarinic DREADD agonist
Chemical Name: 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews (1)
Literature

Biological Activity

Potent muscarinic DREADD agonist (pEC50 values are 8.91, 8.48 and 7.77 for hM1Dq, hM3Dq and hM4Di in vitro, respectively). Exhibits > 10-fold higher affinity for hM1Dq and hM4Di compared to wild type receptors. Also displays little to no activity at wild type M3 receptors. Activates neurons expressing hM3Dq DREADDS and inhibits activity in neurons expressing hM4Di in vivo. Displays excellent brain permeability. Water soluble salt also available, DREADD agonist 21 hydrochloride (Cat. No. 6422).

Technical Data

M. Wt 278.35
Formula C17H18N4
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 56296-18-5
PubChem ID 11818276
InChI Key JCBYXNSOLUVGTF-UHFFFAOYSA-N
Smiles C1(N4CCNCC4)=NC(C=CC=C3)=C3NC2=C1C=CC=C2

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 27.84 100
ethanol 27.84 100

Preparing Stock Solutions

The following data is based on the product molecular weight 278.35. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.59 mL 17.96 mL 35.93 mL
5 mM 0.72 mL 3.59 mL 7.19 mL
10 mM 0.36 mL 1.8 mL 3.59 mL
50 mM 0.07 mL 0.36 mL 0.72 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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

Chen et al (2015) The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem.Neurosci. 18 476 PMID: 25587888

Thompson et al (2018) DREADD agonist 21 (C21) is an effective agonist for muscarinic-based DREADDs in vitro and in vivo. ACS Pharmacol.Transl.Sci.


If you know of a relevant reference for DREADD agonist 21, please let us know.

Keywords: DREADD agonist 21, DREADD agonist 21 supplier, designer, receptors, drugs, DREADDs, hM3Dq, muscarinic, compound, 21, C21, Non-selective, Muscarinics, 5548, Tocris Bioscience

Citations for DREADD agonist 21

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Reviews for DREADD agonist 21

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Used in place of CNO
By Anonymous on 12/01/2017
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: Brain tissue

Used this product in place of CNO


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GPCR

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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.