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GSK682753A研究進(jìn)展

發(fā)布日期：2017-10-27   瀏覽次數(shù)：0
核心提示：a href=https://www.medchemexpress.com/GSK682753A.htmlGSK682753A/a產(chǎn)品描述：GSK682753A is a selective and highly potent i
<a href="https://www.medchemexpress.com/GSK682753A.html">GSK682753A</a>產(chǎn)品描述：GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (<b>EBI2</b>) with an <b>IC<sub>50</sub></b> of 53.6 nM.


IC50 & Target: IC50: 53.6 nM (EBI2)<sup>[1]</sup>

<i><b>In Vitro:</b></i> GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibition of G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-response element-binding protein-based reporter and guanosine5'-3-O-(thio)-triphosphate (GTPγS) binding assays, the potency of this compound is 2.6-53.6 nM, and its inhibitory efficacy is 75%. GSK682753A dose-dependently inhibits EBI2 with an IC<sub>50</sub>of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPγS binding, and cAMP-response element-binding protein activation with similar potency<sup>[1]</sup>.

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