JHU 37160

Catalog # Availability Size / Price Qty
7198/10
7198/50
JHU 37160 | CAS No. 2369979-68-8 | DREADD Activators
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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)-4-fluoro-5H-dibenzo[b,e][1,4]diazepine

Purity: ≥98%

Product Details
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Biological Activity

JHU 37160 is a high affinity and highly potent activator of hM3Dq and hM4Di DREADDs (Ki values are 1.9 nM and 3.6 nM for hM3Dq and hM4Di in vitro, respectively; EC50 values are 0.2 nM and 18.5 nM for hM4Di and hM3Dq in vitro, respectively). Displays approximately 25-fold higher affinity for hM4Di compared to DREADD agonist 21 (Cat. No. 5548). 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, and increases hM3Dq-stimulated locomotion in rats expressing hM3Dq in TH-expressing neurons. Brain penetrant in mice, rats and non-human primates.

Technical Data

M.Wt:
358.85
Formula:
C19H20ClFN4
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at RT
CAS No:
2369979-68-8

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.

Background References

  1. High-potency ligands for DREADD imaging and activation in rodents and monkeys.
    Bonaventura et al.
    Nat.Commun., 2019;10:4627

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