Identification | Back Directory | [Name]
N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide | [CAS]
1428327-31-4 | [Synonyms]
JNJ-479655 JNJ-47965567 JNJ-47965567 >=98% (HPLC) JNJ-47965567
(JNJ47965567) N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE 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 3-Pyridinecarboxamide, 2-(phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]- | [Molecular Formula]
C28H32N4O2S | [MDL Number]
MFCD28334214 | [MOL File]
1428327-31-4.mol | [Molecular Weight]
488.64 |
Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMF:30.0(Max Conc. mg/mL);61.39(Max Conc. mM) DMSO:59.62(Max Conc. mg/mL);122.01(Max Conc. mM) DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.51(Max Conc. mM) Ethanol:12.5(Max Conc. mg/mL);25.58(Max Conc. mM) | [form ]
powder | [color ]
white to beige |
Hazard Information | Back Directory | [Description]
JNJ-47965567 is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux, which is reduced by JNJ-47965567 in 1321N1 cells transfected with recombinant P2X7 human, macaque, dog, rat, or mouse protein with pIC50s of 8.3, 8.6, 8.5, 7.2, or 7.5, respectively. JNJ-47965567 suppresses neonatal hypoxia-induced seizures in mice and has some anticonvulsant properties in rats. It also reduces spontaneous seizures in epileptic mice even after treatment is stopped. | [Uses]
2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]-3-pyridinecarboxamide is a potent and selective human P2X7 antagonist. | [Biochem/physiol Actions]
JNJ-47965567 is a potent P2X7 antagonist with high affinity for the rat receptor (pKi = 8.7). It is centrally available after systemic injection with a superior brain:plasma distribution compared to other available P2X7 antagonists. JNJ-47965567 was shown to suppress epileptic seizures in a mouse model of epilepsy. It appears to have a disease modifying effect since spontaneous seizure rates did not increase once treatment with JNJ-477965567 was stopped. | [storage]
Store at +4°C |
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BOC Sciences
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Sigma-Aldrich
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DC Chemicals
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