JHU37152

Catalog No.S9789 Batch:S978901

Technical Data

Formula	C₁₉H₂₀ClFN₄
Molecular Weight	358.84	CAS No.	2369979-67-7
Solubility (25°C)*	In vitro	DMSO	72 mg/mL (200.64 mM)
		Ethanol	24 mg/mL (66.88 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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]

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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).
Animal Study:^{^[1]}	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

Cell Assay:^{^[1]}

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).

Animal Study:^{^[1]}

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

References

[1] Jordi Bonaventura, et al. Nat Commun. 2019 Oct 11;10(1):4627.

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SHIPPING AND STORAGE
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