JNJ-63533054

JNJ-63533054 is a potent, selective and orally active GPR139 agonist with an EC50 of 16 nM for human GPR139 (hGPR139) . JNJ-63533054 shows selective for GPR139 over other GPCRs, ion channels, and transporters. JNJ-63533054 can cross the blood-brain barrier (BBB) [1][2].

Product Specifications

CAS Number

[1802326-66-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

GPR139

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/JNJ-63533054.html

Purity

99.80

Solubility

DMSO : ≥ 50 mg/mL

Smiles

O=C(NCC(N[C@H](C1=CC=CC=C1)C)=O)C2=CC=CC(Cl)=C2

Molecular Formula

C17H17ClN2O2

Molecular Weight

316.78

Precautions

H302, H315, H319

References & Citations

[1]Dvorak CA, et al. Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor. ACS Med Chem Lett. 2015 Jul 20;6 (9) :1015-8.|[2]Liu C, et al. GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine. Mol Pharmacol. 2015 Nov;88 (5) :911-25.