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JHU37152 AChR agonist

Cat.No.S9789

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
JHU37152 AChR agonist Chemical Structure

Chemical Structure

Molecular Weight: 358.84

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Quality Control

Batch: S978901 DMSO]72 mg/mL]false]Ethanol]24 mg/mL]false]Water]Insoluble]false Purity: 99.79%
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  • COA
  • NMR
  • HPLC
  • SDS
  • Datasheet
99.79

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (200.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble

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Dilution Calculator Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 358.84 Formula

C19H20ClFN4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2369979-67-7 -- Storage of Stock Solutions

Synonyms N/A Smiles CCN1CCN(CC1)C2=NC3=CC(=CC=C3NC4=CC=CC(=C24)F)Cl

Mechanism of Action

Targets/IC50/Ki
hM4Di
(Cell-free assay)
0.5 nM(EC50)
hM3Dq
(Cell-free assay)
1.8 nM(Ki)
hM3Dq
(Cell-free assay)
5 nM(EC50)
hM4Di
(Cell-free assay)
8.7 nM(Ki)
In vitro

This compound is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.
In vivo

JHU37152 exhibits high in vivo DREADD potency. This compound exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.
References

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