GSK682753ACAS号: 1334294-76-6分子式: C23H21Cl3N2O3分子量: 479.78描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)参考文献
产品描述 | |
描述 |
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO: ≥ 27 mg/mL
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生物活性 | |
靶点 |
EBI2_GPR183
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In vitro(体外研究) |
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 IC50of 53.6 nM. GSK682753A inhibits ERK phosphorylation, GTPγS binding, and cAMP-response element-binding protein activation with similar potency.
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参考文献 | |
参考文献 |
[1]. Benned-Jensen T, et al. Ligand modulation of the Epstein-Barr virus-induced seven-transmembrane receptor EBI2: identification of a potent and efficacious inverse agonist. J Biol Chem. 2011 Aug 19;286(33):29292-302.
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分子结构图