ChemicalBook > CAS DataBase List > N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

Product Name: N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide
CAS No.: 1428327-31-4
Chemical Name: N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide
Synonyms: JNJ-47965567;JNJ-479655;JNJ-47965567 >=98% (HPLC);JNJ-47965567, 10 mM in DMSO;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;Inhibitor,P2X7,JNJ-47965567,pain,JNJ 47965567,P2X Receptor,inhibit,neuropathic,JNJ47965567,P2XRs;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]-
CBNumber: CB83146923
Molecular Formula: C28H32N4O2S
Formula Weight: 488.64
MOL File: 1428327-31-4.mol

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N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1708
Product name: JNJ-47965567
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $132
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML1708
Product name: JNJ-47965567
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $538
Updated: 2025/07/31

Cayman Chemical

Product number: 21895
Product name: JNJ-47965567
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 21895
Product name: JNJ-47965567
Purity: ≥98%
Packaging: 5mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 21895
Product name: JNJ-47965567
Purity: ≥98%
Packaging: 10mg
Price: $199
Updated: 2024/03/01

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N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide Chemical Properties,Usage,Production

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.

in vivo

JNJ-47965567 (30-100 mg/kg; s.c.) attenuates IL-1β release induced by Bz-ATP^[1].
JNJ-47965567 (30 mg/kg) attenuates amphetamine-induced hyperactivity and exhibits modest, yet significant efficacy in the rat model of neuropathic pain^[1].

Animal Model:	Male Sprague Dawley rats^[1]
Dosage:	30 mg/kg, 100 mg/kg
Administration:	Subcutaneous injection; 30 minutes prior to Bz-ATP infusion
Result:	Significantly attenuated IL-1β release at 100 mg/kg, with no effect at 30 mg/kg dose group.

IC 50

P2X7 Receptor

storage

Store at +4°C

References

[1] ANINDYA BHATTACHARYA. Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567[J]. British Journal of Pharmacology, 2013, 170 3: 624-640. DOI: 10.1111/bph.12314
[2] NATALIA RODRIGUEZ-ALVAREZ . Effects of P2X7 receptor antagonists on hypoxia-induced neonatal seizures in mice[J]. Neuropharmacology, 2017, 116: Pages 351-363. DOI: 10.1016/j.neuropharm.2017.01.005
[3] WOLFGANG FISCHER. Critical Evaluation of P2X7 Receptor Antagonists in Selected Seizure Models.[J]. PLoS ONE, 2016: e0156468. DOI: 10.1371/journal.pone.0156468
[4] ALBA JIMENEZ-PACHECO. Transient P2X7 Receptor Antagonism Produces Lasting Reductions in Spontaneous Seizures and Gliosis in Experimental Temporal Lobe Epilepsy.[J]. Journal of Neuroscience, 2016, 36 22: 5920-5932. DOI: 10.1523/jneurosci.4009-15.2016

N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide Preparation Products And Raw materials

Raw materials

Preparation Products

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N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide Suppliers

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1428327-31-4, N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamideRelated Search:

N-ACETYLLACTOSAMINE

JNJ-479655

N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE

JNJ-47965567

N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

JNJ-47965567 (JNJ47965567)

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]-

JNJ-47965567 >=98% (HPLC)

Inhibitor,P2X7,JNJ-47965567,pain,JNJ 47965567,P2X Receptor,inhibit,neuropathic,JNJ47965567,P2XRs

JNJ-47965567, 10 mM in DMSO

1428327-31-4