JHU 37160

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Cat.No. 7198 - JHU 37160 | C19H20ClFN4 | CAS No. 2369979-68-8
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% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity

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 18.5 nM and 0.2 nM for hM3Dq and hM4Di 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
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 2369979-68-8
PubChem ID 139033723
InChI Key SWSCWOSASZXIRK-UHFFFAOYSA-N
Smiles CCN1CCN(C2=NC3=CC(Cl)=CC=C3NC4=C(C=CC=C24)F)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 17.94 50

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
0.5 mM 5.57 mL 27.87 mL 55.73 mL
2.5 mM 1.11 mL 5.57 mL 11.15 mL
5 mM 0.56 mL 2.79 mL 5.57 mL
25 mM 0.11 mL 0.56 mL 1.11 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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Keywords: JHU 37160, JHU 37160 supplier, JHU37160, DREADD, agonist, agonists, activator, activators, acutator, muscarinic, hM3Dq, hM4Di, brain, penetrant, DREADDs, 7198, Tocris Bioscience

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Literature in this Area

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