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

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

中文名称N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE
中文同义词化合物JNJ-47965567;N-((4-(4-苯基哌嗪-1-基)四氢-2H-吡喃-4-基)甲基)-2-(苯硫基)烟酰胺;JNJ 47965567,P2X7拮抗剂
英文名称N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide
英文同义词N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide;JNJ-479655;N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE;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);JNJ-47965567
CAS号1428327-31-4
分子式C28H32N4O2S
分子量488.64
EINECS号
相关类别
Mol文件1428327-31-4.mol
结构式N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE 结构式

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

储存条件2-8°C
溶解度DMF:30.0(最大浓度 mg/mL);61.39(最大浓度 mM)
DMSO:59.62(最大浓度 mg/mL);122.01(最大浓度 mM)
DMSO:PBS ( pH 7.2) (1:3):0.25(最大浓度 mg/mL);0.51(最大浓度 mM)
乙醇:12.5(最大浓度 mg/mL);25.58(最大浓度 mM)
形态粉末
颜色白色至米色

N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE 用途与合成方法

JNJ-47965567 是一种中枢通透性、高亲和力、选择性的 P2X7 拮抗剂,对人和大鼠 P2X7 作用的 pKi 值分别为 7.9 和 8.7。JNJ-47965567 可用于探讨中枢 P2X7 在中枢神经系统病理生理模型中的作用。

pKi: 7.9 (huaman P2X7), 8.7 (rat P2X7)

JNJ-47965567 exhibits high affinity for human and rat P2X7 in membrane preparations of 1321N1 cells.
JNJ-47965567 does not block IL-6 and TNF-α release, under identical conditions (LPS and BZ-ATP) used for IL-1β and IL-18 release.
JNJ-47965567 attenuates IL-1β release with pIC 50 s of 6.7 ± 0.07 (human blood), 7.5 ± 0.07 (human monocytes) and 7.1 ± 0.1 (rat microglia), respectively, in native systems.

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

Animal Model: Male Sprague Dawley rats
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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-101418N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE
JNJ-47965567
1428327-31-410mM * 1mLin DMSO806元
2024/04/30HY-101418N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE
JNJ-47965567
1428327-31-410mg1200元

N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE 上下游产品信息

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