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 > IC-87201
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:
 
IC-87201
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。
IC-87201图片
CAS NO:866927-10-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 309.15
FormulaC13H10Cl2N4O
CAS No. 866927-10-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 28 mg/mL
Water: N/A
Ethanol: N/A
SMILES OC1=C(Cl)C=C(Cl)C=C1CNC2=CC=C(NN=N3)C3=C2
Synonyms IC87201; IC-87201; IC 87201
实验参考方法
In Vitro

In vitro activity: IC87201 (10 and 100 nM) attenuats NMDA/glycine-induced decreases in neurite outgrowth. IC87201 dose-dependently reduces NMDA-induced cGMP production in primary hippocampal neurons (DIV 14-21) with an IC50 of 2.7 μM. IC87201 increases the number of branches at 10-30 μM when compared to control-treated neurons. IC87201 (20 μM) suppresses NMDA-stimulated cGMP formation relative to vehicle, in cultured hippocampal neurons. IC87201 (500-1800 μM) does not inhibit any of the probe-PDZ interactions involving PDZ1, PDZ2, PDZ3 of PSD-95 or nNOS-PDZ, or bind the canonical PDZ ligand binding sites. IC87201 binds to the β-finger of nNOS-PDZ and allosterically inhibits the nNOS-PDZ/PSD-95-PDZ interactions. IC87201 shows high degree of fluorescence-based artefactual signal when using TAMRA-nNOS as probe.


Kinase Assay: IC87201 (500-1800 μM) does not inhibit any of the probe-PDZ interactions involving PDZ1, PDZ2, PDZ3 of PSD-95 or nNOS-PDZ, or bind the canonical PDZ ligand binding sites. IC87201 binds to the β-finger of nNOS-PDZ and allosterically inhibits the nNOS-PDZ/PSD-95-PDZ interactions. IC87201 shows high degree of fluorescence-based artefactual signal when using TAMRA-nNOS as probe.


Cell Assay:

In VivoIC87201 (1 mg/kg) is effective in treating NMDA-induced thermal hyperalgesia in mice, with a corresponding peak plasma level of 55 ng/mL (or 0.2 μM). IC87201 (1, 4 and 10 mg/kg, i.p.) does not produce impairment in either spatial working memory or source memory.
Animal model Mice with NMDA-induced thermal hyperalgesia
Formulation & Dosage1, 4 and 10 mg/kg, i.p.
References Sci Rep. 2015 Jul 16;5:12157.Neuroscience. 2015 Aug 20;301:421-38.Behav Brain Res. 2016 May 15;305:23-9.