ChemicalBook > CAS DataBase List > 5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-

5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-

Product Name
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-
CAS No.
2369979-68-8
Chemical Name
5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-
Synonyms
JHU37160, 10 mM in DMSO;8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-5H-Dibenzo[b,e][1,4]diazepine;5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-;Inhibitor,hM4Di,Clozapine,hM3Dq,DREADD,inhibit,Muscarinic acetylcholine receptor,JHU-37160,JHU37160,mAChR
CBNumber
CB78236811
Molecular Formula
C19H20ClFN4
Formula Weight
358.84
MOL File
2369979-68-8.mol
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5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro- Property

Boiling point:
493.0±55.0 °C(Predicted)
Density 
1.34±0.1 g/cm3(Predicted)
storage temp. 
Store at RT
solubility 
DMSO|17.94|50|
pka
7.63±0.10(Predicted)
form 
solid
color 
Yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML3466
Product name
JHU37160
Purity
≥98% (HPLC)
Packaging
5mg
Price
$87.3
Updated
2025/07/31
Sigma-Aldrich
Product number
SML3466
Product name
JHU37160
Purity
≥98% (HPLC)
Packaging
25mg
Price
$370
Updated
2025/07/31
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5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro- Chemical Properties,Usage,Production

Uses

JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5?nM and 0.2?nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue[1].

Biological Activity

JHU37160 (J60) is a potent DREADDs (Designer Receptors Exclusively Activated by Designer Drugs) ligand (hM3Dq/hM4Di Ki = 1.9/3.6 nM using mouse brain tissue, 18.5/0.2 nM by celluar BRET assays) with ~25-fold improved affinity than C21 and high in vivo potency for CNS applications. J60 selectively competes against clozapine at DREADDs, but not other clozapine-binding sites in mouse brain tissue ex vivo (10 nM), increases hM3Dq-stimulated locomotion in TH-hM3Dq rats (0.01-0.3 mg/kg i.p.) and selectively inhibits locomotor activity of D1-hM3Dq and D1-hM4Di transgenic, but not wild-type, mice (0.01-1 mg/kg i.p.).

in vivo

JHU37160 (0.1 mg/kg; i.p.) exhibits high DREADD occupancy in mice and rats[1].
JHU37160 (0.01-1 mg/kg; i.p.) selectively inhibits locomotor activity in D1-hM3Dq and D1-hM4Di mice without any significant locomotor effects observed in WT mice[1].

IC 50

mAChR3; mAChR4

storage

Room temperature

References

[1] Bonaventura J, et, al. High-potency ligands for DREADD imaging and activation in rodents and monkeys. Nat Commun. 2019 Oct 11;10(1):4627. DOI:10.1038/s41467-019-12236-z

5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro- Preparation Products And Raw materials

Raw materials

Preparation Products

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5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro- Suppliers

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2369979-68-8, 5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-Related Search:

5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-1-fluoro-

  • 5H-Dibenzo[b,e][1,4]diazepine, 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-
  • 8-chloro-11-(4-ethyl-1-piperazinyl)-4-fluoro-5H-Dibenzo[b,e][1,4]diazepine
  • Inhibitor,hM4Di,Clozapine,hM3Dq,DREADD,inhibit,Muscarinic acetylcholine receptor,JHU-37160,JHU37160,mAChR
  • JHU37160, 10 mM in DMSO
  • 2369979-68-8