JNJ-47965567 ≥98%
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| 包装规格: | 25mg 100mg 250mg 1g in glass bottle |
| 溶解性: | 溶于DMSO(20mg/ml) |
| 产品描述: | 基本信息 产品编号: J10056 产品名称: JNJ-47965567 CAS: 1428327-31-4 储存条件 粉末 -20℃ 四年 分子式: C28H32N4O2S 溶于液体 -80℃ 6个月 分子量: 488.64 -20℃ 1个月 化学名: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide Solubility (25°C): 体外: DMSO Ethanol Water 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.0465mL 10.2325mL 10.2325mL 5mM 0.4093mL 2.0465mL 4.0930mL 10mM 0.2046mL 1.0232mL 2.0465mL 生物活性 产品描述 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。 靶点 pKi:7.9 (huaman P2X7),8.7 (rat P2X7) 体外研究 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-1βand IL-18 release.JNJ-47965567 attenuates IL-1βrelease with pIC50s of 6.7±0.07 (human blood),7.5±0.07 (human monocytes) and 7.1±0.1 (rat microglia),respectively,in native systems. 体内研究 JNJ-47965567 (30-100mg/kg;s.c.) attenuates IL-1β release induced by Bz-ATP.JNJ-47965567 (30mg/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: 30mg/kg,100mg/kg Administration: Subcutaneous injection;30 minutes prior to Bz-ATP infusion Result: Significantly attenuated IL-1β release at 100mg/kg,with no effect at 30mg/kg dose group. |
| 保存条件: | -20℃ |
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