JHU37160

Catalog No.S9790 Batch:S979001

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Technical Data

Formula

C19H20ClFN4

Molecular Weight 358.84 CAS No. 2369979-68-8
Solubility (25°C)* In vitro DMSO 72 mg/mL (200.64 mM)
Ethanol 72 mg/mL (200.64 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.)

Preparing Stock Solutions

Biological Activity

Description JHU37160 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.9 nM and 3.6 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 18.5 nM and 0.2 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)
hM4Di [1]
(Cell-free assay)
hM3Dq [1]
(Cell-free assay)
0.2 nM(EC50) 1.9 nM(Ki) 3.6 nM(Ki) 18.5 nM(EC50)
In vitro

JHU37160 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

JHU37160 exhibits high in vivo DREADD potency. JHU37160 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 JHU37160 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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.