1428327-31-4

1428327-31-4 structure

Name: JNJ 47965567
Chemical Name: JNJ-47965567
CAS Number: 1428327-31-4
Molecular Formula: C₂₈H₃₂N₄O₂S
Molecular Weight: 488.644
Catalog: Signaling Pathways Membrane Transporter/Ion Channel P2X Receptor
Create Date: 2020-01-11 16:58:49
Modify Date: 2024-04-03 12:23:47
JNJ-47965567 is a potent, selective, centrally permeable P2X7 receptor antagonist with pKi of 7.9 and 8.7 for human and rat P2X7, respectively; attenuates IL-1β release with pEC50 of 6.7 (human blood), 7.5 (human monocytes) and 7.1 (rat microglia); exhibits target engagement in rat brain with brain EC50 of 78 ± 19 ng/ml, as well as functional block of Bz-ATP induced IL-1β release; attenuateas amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain.

Name	JNJ-47965567
Synonyms	MFCD28334214 2-(phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]-3-pyridinecarboxamide N-{[4-(4-Phenyl-1-piperazinyl)tetrahydro-2H-pyran-4-yl]methyl}-2-(phenylsulfanyl)nicotinamide JNJ-47965567 3-Pyridinecarboxamide, 2-(phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]-

Description	JNJ-47965567 is a potent, selective, centrally permeable P2X7 receptor antagonist with pKi of 7.9 and 8.7 for human and rat P2X7, respectively; attenuates IL-1β release with pEC50 of 6.7 (human blood), 7.5 (human monocytes) and 7.1 (rat microglia); exhibits target engagement in rat brain with brain EC50 of 78 ± 19 ng/ml, as well as functional block of Bz-ATP induced IL-1β release; attenuateas amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain.
References	References 1. Bhattacharya A, et al. Br J Pharmacol. 2013 Oct;170(3):624-40. 2. Jimenez-Pacheco A, et al. J Neurosci. 2016 Jun 1;36(22):5920-32. 3. Letavic MA, et al. ACS Med Chem Lett. 2013 Mar 12;4(4):419-22. 4. Rodriguez-Alvarez N, et al. Neuropharmacology. 2017 Apr;116:351-363. View Related Products by Target P2X Receptor