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GSK682753A

CAS No. : 1334294-76-6

MCE 站：GSK682753A

产品活性：GSK682753A是EB病毒诱导受体2 (EBI2) 的反向激动剂, IC₅₀值为 53.6 nM。

研究领域：GPCR/G Protein

作用靶点：EBI2/GPR183

In Vitro: 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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