JHU 37152

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Cat.No. 7197 - JHU 37152 | C19H20ClFN4 | CAS No. 2369979-67-7
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% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

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.

Technical Data

M. Wt 358.85
Formula C19H20ClFN4
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 2369979-67-7
PubChem ID 139033721
InChI Key NZMZJNNWMSYDNX-UHFFFAOYSA-N
Smiles CCN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=CC=CC(F)=C24)CC1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.88 100
ethanol 35.88 100

Preparing Stock Solutions

The following data is based on the product molecular weight 358.85. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.79 mL 13.93 mL 27.87 mL
5 mM 0.56 mL 2.79 mL 5.57 mL
10 mM 0.28 mL 1.39 mL 2.79 mL
50 mM 0.06 mL 0.28 mL 0.56 mL

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References

References are publications that support the biological activity of the product.

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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Literature in this Area

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