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Submit ReviewJHU 37152
Description: High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant
Chemical Name: 8-Chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine
Purity: ≥98% (HPLC)
Biological Activity for JHU 37152
JHU 37152 is a high affinity and highly potent activator of hM3Dq and hM4Di DREADDs (Ki values are 1.8 nM and 8.7 nM for hM3Dq and hM4Di in vitro, respectively; EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in vitro, respectively). Selectively displaces [3H]clozapine from DREADDs in vivo, but not from other clozapine binding sites. Inhibits locomotor activity in mice expressing hM3Dq and hM4Di in D1-expressing neurons. Brain penetrant in mice, rats and non-human primates.
Technical Data for JHU 37152
| M. Wt | 358.85 |
| Formula | C19H20ClFN4 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 2369979-67-7 |
| PubChem ID | 139033721 |
| InChI Key | NZMZJNNWMSYDNX-UHFFFAOYSA-N |
| Smiles | CCN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC(F)=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 JHU 37152
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.88 | 100 | |
| ethanol | 35.88 | 100 |
Preparing Stock Solutions for JHU 37152
The following data is based on the product molecular weight 358.85. 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 | 2.79 mL | 13.93 mL | 27.87 mL |
| 5 mM | 0.56 mL | 2.79 mL | 5.57 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.79 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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Product Datasheets for JHU 37152
References for JHU 37152
References are publications that support the biological activity of the product.
Bonaventura et al (2019) High-potency ligands for DREADD imaging and activation in rodents and monkeys. Nat.Commun. 10 4627 PMID: 31604917
If you know of a relevant reference for JHU 37152, please let us know.
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Keywords: JHU 37152, JHU 37152 supplier, JHU37152, DREADD, agonist, agonists, activator, activators, actuator, muscarinic, hM3Dq, hM4Di, brain, penetrant, DREADDs, 7197, Tocris Bioscience
Citations for JHU 37152
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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.