JHU 37152

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.

Product information

CAS Number: 2369979-67-7

Molecular Weight: 358.84

Formula: C19H20ClFN4

Synonym:

JHU-37152

JHU37152

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

Smiles: CCN1CCN(CC1)C1=NC2=CC(Cl)=CC=C2NC2=CC=CC(F)=C21

InChiKey: NZMZJNNWMSYDNX-UHFFFAOYSA-N

InChi: InChI=1S/C19H20ClFN4/c1-2-24-8-10-25(11-9-24)19-18-14(21)4-3-5-16(18)22-15-7-6-13(20)12-17(15)23-19/h3-7,12,22H,2,8-11H2,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. 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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