JNJ 63533054

Catalog No.S6425 Batch:S642501

Print

Technical Data

Formula

C17H17ClN2O2
Molecular Weight 316.78 CAS No. 1802326-66-4
Solubility (25°C)* In vitro DMSO 63 mg/mL (198.87 mM)
 
 
* <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 JNJ 63533054 is a potent and selective GPR139 agonist. It specifically activated human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays.
Targets
human GPR139 [1]
(Cell-free assay)		 mouse GPR139 [1]
(Cell-free assay)		 rat GPR13 [1]
(Cell-free assay)
0.024 μM(Ki) 0.054 μM(Ki) 0.075 μM(Ki)
In vitro

JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM)[1].
In vivo

The small-molecule JNJ-63533054 is found to be devoid of any cross-reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters, and it displays suitable pharmacokinetic properties for in vivo studies. JNJ-63533054 crosses the rat blood-brain barrier after oral administration and achieves exposure in the micromolar range. JNJ-63533054 administration decreases spontaneous locomotor activity in rats[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    male Sprague-Dawley rats (350-450 g)

  • Dosages

    3, 10, and 30 mg/kg

  • Administration

    oral

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.