您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > JNJ-55308942
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
JNJ-55308942
本产品不向个人销售,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-55308942图片
CAS NO:2166558-11-6
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
JNJ-55308942 是 P2X7 功能性的选择性脑渗透拮抗剂,对 hP2X7 和 rP2X7 的 IC50 分别为 10 和 15 nM,Kis 分别为 7.1 和 2.9 nM。

产品描述

JNJ-55308942 is a selective and brain-penetrant antagonist of P2X7 functional with IC50s of 10 and 15 nM and Kis of 7.1 and 2.9 nM for hP2X7 and rP2X7, respectively.

体外活性

JNJ-55308942 shows pKis of 8.1and 8.5 for recombinant hP2X7 and rP2X7. JNJ-55308942 attenuates IL-1β release in a concentration-dependent manner in human blood and in mouse blood and microglia[2].

体内活性

JNJ-55308942 (5 mg/kg; p.o.) shows the F of 81%, Vss of 1.7 L/kg, CL of 1.7 L/kg, Cmax of 3.7 mL min/kg, and AUC of 1747 ng/mL[1]. In male C57/BL6J mice, JNJ-55308942 (30 mg/kg; p.o.) significantly attenuates the effect of LPS on FSC, CD45 surface expression, and CD11b surface expression. In a model of Bacillus Calmette-Guerin-induced depression, JNJ-55308942 (30 mg/kg; orally) reverses the BCG-induced deficits of sucrose preference and social interaction (ED50 = 0.07 mg/kg). The P2X7 antagonist (3 mg/kg, orally) blocks Bz-ATP-induced brain IL-1β release in conscious rats[2].

Cas No.

2166558-11-6

分子式

C17H12F5N7O

分子量

425.32

储存和溶解度

DMSO:90mg/mL (211.6mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years