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JNJ-54166060
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
JNJ-54166060图片
CAS NO: 1627900-41-7
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
JNJ-54166060 是一种 P2X7 受体 ( P2X7 receptor) 拮抗剂，对人/大鼠/小鼠 P2X7 受体作用的 IC50值分别为 4/115/72 nM。
生物活性

JNJ-54166060 is a potent and selectiveP2X7 receptorantagonist, withIC50s of 4/115/72 nM for human/rat/mouseP2X7 receptor, respectively[1].
IC50& Target

IC50: 4/115/72 nM (human/rat/mouse P2X7 receptor)[1]
体内研究
(In Vivo)

JNJ-54166060 exhibits high oral bioavailability (rat 55%, dog >100%, monkey 54 %) and Cmax(rat 375, dog 1249, monkey 389 ng/mL) following oral administration (rat 5 and, dog 5 mg/kg, monkey 5 mg/kg)[1].
JNJ-54166060 exhibits terminal elimination half-lives (rat 1.7 and, dog 11.9 h, monkey 4.2 h) due to low-moderate clearance (30, 5.5, and 14 mL/min/kg respectively) following intravenous administration (rat 1.0 and, dog 1.0 mg/kg, monkey 1.0 mg/kg)[1].

Animal Model: Sprague-Dawley rats[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (55%), Cmax(375 ng/mL), T1/2(1.7 h).
Animal Model: Beagle dogs[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (>100%), Cmax(1249 ng/mL), T1/2(11.9 h).
Animal Model: Cynomolgus monkeys[1]
Dosage: 1 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: Oral bioavailability (54%), Cmax(389 ng/mL), T1/2(4.2 h).
分子量

438.81
Formula

C20H15ClF4N4O
CAS 号

1627900-41-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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