1428327-31-4
中文名稱
N-[[4-(4-PHENYLPIPERAZIN-1-YL)OXAN-4-YL]METHYL]-2-PHENYLSULFANYLPYRIDINE-3-CARBOXAMIDE
英文名稱
N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide
CAS
1428327-31-4
分子式
C28H32N4O2S
分子量
488.64
MOL 文件
1428327-31-4.mol
更新日期
2024/12/10 17:13:38
1428327-31-4 結(jié)構(gòu)式
基本信息
中文別名
化合物JNJ-47965567 英文別名
JNJ-479655JNJ-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]-
物理化學性質(zhì)
儲存條件2-8°C
溶解度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)
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)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
JNJ-47965567 是一種中樞通透性、高親和力、選擇性的 P2X7 拮抗劑，對人和大鼠 P2X7 作用的 pKi 值分別為 7.9 和 8.7。JNJ-47965567 可用于探討中樞 P2X7 在中樞神經(jīng)系統(tǒng)病理生理模型中的作用。靶點
pKi: 7.9 (huaman P2X7), 8.7 (rat P2X7)
體外研究
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.
體內(nèi)研究
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. |