JHU 37152

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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)
Literature (3)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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

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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

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

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

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.