Home Neuronal Signaling AChR agonist JHU37152 For research use only.

JHU37152

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 Chemical Structure

JHU37152 Chemical Structure

CAS: 2369979-67-7

Purity & Quality Control

Batch: S978901 DMSO] 72 mg/mL] false] Ethanol] 24 mg/mL] false] Water] Insoluble] false Purity: 99.79%
99.79

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Biological Activity

Description 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.
Targets
hM4Di [1]
(Cell-free assay)		 hM3Dq [1]
(Cell-free assay)		 hM3Dq [1]
(Cell-free assay)		 hM4Di [1]
(Cell-free assay)
0.5 nM(EC50) 1.8 nM(Ki) 5 nM(EC50) 8.7 nM(Ki)
In vitro
In vitro

JHU37152 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.[1]
Cell Research Cell lines HEK-293 cells
Concentrations --
Incubation Time 250 s
Method

HEK-293 cells are transfected with 7 µg/dish of the cDNA encoding for hM3Dq or hM4Di and 7 µg/dish of GCaMP6. 48 hours after transfection, cells are harvested, washed, resuspended in Mg2+-free Locke's buffer pH 7.4 containing 5.6  mM of glucose and approximately 200,000 cells/well are distributed in black 96-well plates. Increasing concentrations of JHU37152 are added to the cells and fluorescence intensity (excitation at 480 nM, emission at 530 nM) is measured at 18-s intervals during 250 s using a PHERAstar FSX. The net change in intracellular Ca2+ concentration is expressed as F − F0 where F is the fluorescence at a given concentration of ligand and F0 is the average of the baseline values (fluorescence values of buffer-treated wells).
In Vivo
In vivo

JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1]
Animal Research Animal Models 6 week-old male wild-type C57BL/6J mice, 6 week-old male Sprague–Dawley rats
Dosages 0.01 mg/kg - 0.3 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 358.84 Formula

C19H20ClFN4
CAS No. 2369979-67-7 SDF --
Smiles CCN1CCN(CC1)C2=NC3=CC(=CC=C3NC4=CC=CC(=C24)F)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 72 mg/mL ( (200.64 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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