JNJ-55308942

JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM) . JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain[1][2].

Product Specifications

CAS Number

[2166558-11-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/jnj-55308942.html

Purity

99.92

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=C(F)C(C(F)(F)F)=NC=C1)N2[C@@H](C)CC(N(C3=NC=C(F)C=N3)N=N4)=C4C2

Molecular Formula

C17H12F5N7O

Molecular Weight

425.32

Precautions

H302, H315, H319, H335

References & Citations

[1]Bhattacharya A, et al. Neuropsychopharmacology of JNJ-55308942: evaluation of a clinical candidate targeting P2X7 ion channels in animal models of neuroinflammation and anhedonia. Neuropsychopharmacology. 2018;43 (13) :2586-2596.|[2]Chrovian CC, et al. A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate. J Med Chem. 2018;61 (1) :207-223.