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
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
N-Bromosuccinimide Price
- Product number
- SML1708
- Product name
- JNJ-47965567
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $132
- Updated
- 2025/07/31
- Product number
- SML1708
- Product name
- JNJ-47965567
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $538
- Updated
- 2025/07/31
- Product number
- 21895
- Product name
- JNJ-47965567
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 21895
- Product name
- JNJ-47965567
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- 21895
- Product name
- JNJ-47965567
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $199
- Updated
- 2024/03/01
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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