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
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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 |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 690.1±55.0 °C at 760 mmHg |
| Molecular Formula | C28H32N4O2S |
| Molecular Weight | 488.644 |
| Flash Point | 371.2±31.5 °C |
| Exact Mass | 488.224609 |
| LogP | 6.50 |
| Vapour Pressure | 0.0±2.2 mmHg at 25°C |
| Index of Refraction | 1.670 |