JHU 37152

Catalog # Availability Size / Price Qty
7197/10
7197/50
JHU 37152 | CAS No. 2369979-67-7 | 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)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine

Purity: ≥98%

Product Details
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Biological Activity

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

M.Wt:
358.85
Formula:
C19H20ClFN4
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at RT
CAS No:
2369979-67-7

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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