JHU 37160


Catalog No. size PriceQuantity
M7151-2 2mg solid $114
M7151-10 10mg solid $436

Description

Cas:2369979-67-7

Product Information:

High affinity and highly potent hM3Dq and hM4Di DREADD agonist; blood brain barrier penetrant.

 

Biological Activity:

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.

 

Chemical Name: 358.85

 

Formula: C19H20ClFN4

 

Storage: Store at RT

 

Purity: ≥98% (HPLC)

 

Chemical Name: 8-Chloro-11-(4-ethylpiperazin-1-yl)-1-fluoro-5H-dibenzo[b,e][1,4]diazepine

 

InChI Key:

NZMZJNNWMSYDNX-UHFFFAOYSA-N

 

Smiles:

CCN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC(F)=C24)CC1

 

 

References

 

  1. Bonaventura et al (2019) High-potency ligands for DREADD imaging and activation in rodents and monkeys. Nat.Commun. 10 4627 PMID: 31604917

 

Products are for research use only. Not for human use.

 

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