JNJ-42253432
目录号: PL08683 纯度: ≥98%
CAS No. :1428327-35-8
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中文名称
JNJ-42253432
英文名称
JNJ-42253432
英文别名
2-methyl-N-([1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide;BDBM50428288
Cas No.
1428327-35-8
分子式
C28H38N4O
分子量
446.63
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
JNJ-42253432 是能透过中枢神经系统的、口服活性的 P2X7 拮抗剂,其对大鼠和人 P2X7 通道的 pKi 值分别为 9.1 和 7.9.
生物活性
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pK i values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.
性状
Solid
体内研究(In Vivo)
When dosed in rats, JNJ-42253432 occupied the brain P2X7 channel with an ED 50 of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED 50 of 10 mg/kg for SERT occupancy. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Brian Lord, et al. Pharmacology of a novel central nervous system-penetrant P2X7 antagonist JNJ-42253432. J Pharmacol Exp Ther. 2014 Dec;351(3):628-41.
溶解度数据
In Vitro: DMSO : 100 mg/mL (223.90 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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