JNJ-54717793

JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL) . The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders[1][2].

Product Specifications

CAS Number

[1628843-99-1]

UNSPSC

12352005

Target

Orexin Receptor (OX Receptor)

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-54717793.html

Purity

98.06

Solubility

DMSO : 240 mg/mL (ultrasonic)

Smiles

O=C(C1=C(C2=NC=CC=N2)C(F)=CC=C1)N3[C@H](CC[C@@H]43)C[C@H]4NC5=CN=C(C(F)(F)F)C=N5

Molecular Formula

C22H18F4N6O

Molecular Weight

458.41

References & Citations

[1]Préville C, et al. Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793. ACS Med Chem Lett. 2020;11 (10) :2002-2009. Published 2020 Apr 27.|[2]Bonaventure P, et al. Evaluation of JNJ-54717793 a Novel Brain Penetrant Selective Orexin 1 Receptor Antagonist in Two Rat Models of Panic Attack Provocation. Front Pharmacol. 2017;8:357. Published 2017 Jun 9.