Lu AF27139

Lu AF27139 is a potent, selective, and orally active antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively) . Lu AF27139 has rodent-active and CNS-penetrant character. Lu AF27139 has the potential for the research of CNS diseases[1].

Product Specifications

CAS Number

[2097117-06-9]

UNSPSC

12352005

Target

P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/lu-af27139.html

Purity

99.71

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

ClC(C=C1)=CC=C1[C@H](N2CCOCC2)CNC(C3=C(C(F)(F)F)N=C(C4=NC=CC=N4)S3)=O

Molecular Formula

C21H19ClF3N5O2S

Molecular Weight

497.92

References & Citations

[1]Hopper AT, et al. Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. J Med Chem. 2021;64 (8) :4891-4902.|[2]Hopper AT, et al. Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139. J Med Chem. 2021 Apr 22;64 (8) :4891-4902.