Cas No.: | 1428327-31-4 |
Chemical Name: | N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide |
Synonyms: | N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide;2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]-3-pyridinecarboxamide;JNJ 47965567;N-{[4-(4-Phenylpiperazin-1-Yl)oxan-4-Yl]methyl}-2-(Phenylsulfanyl)pyridine-3-Carboxamide;P2X Antagonist III;antagonist JNJ47965567;GTPL7538;JNJ47965567;Z2235332565;N-[[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methyl]-2-phenylsulfanylpyridine-3-carboxamide;N-[[4-(4-phenylp;JNJ-47965567 |
SMILES: | C1=CC=C(C=C1)SC2C(=CC=CN=2)C(=O)NCC3(CCOCC3)N4CCN(CC4)C5=CC=CC=C5 |
Formula: | C28H32N4O2S |
M.Wt: | 488.6443 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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 |