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JNJ-61432059
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-61432059图片
CAS NO:2035814-50-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
JNJ-61432059是具有口服活性的、选择性的AMPAR的负向调节剂,其对GluA1/γ-8的pIC50值为9.7。在老鼠的海马体中显示出具有时间和剂量依赖性的AMPA受体占用情况,在角膜点燃癫痫动物模型中显示出较强的保护作用。
Cas No.2035814-50-5
Canonical SMILESOC1CCN(C2=NC=CC3=C(C4=CC=C(NC(C5)=O)C5=C4)C(C6=CC=C(F)C=C6)=NN32)CC1
分子式C25H22FN5O2
分子量443.47
溶解度DMSO: 50 mg/mL (112.75 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models[1]. pIC50: 9.7 (AMPAR)[1].

[1]. Savall BM, et al. Discovery of Imidazo[1,2-a]pyrazines and Pyrazolo[1,5-c]pyrimidines as TARP γ-8 Selective AMPAR Negative Modulators. ACS Med Chem Lett. 2018 Dec 26;10(3):267-272.