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Description: TG4-155 is a novel, potent and brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 uM) and a panel of other receptors and channels.It blocks the induced expression of inflammatory markers in microglial cells treated with the selective EP2 agonist butaprost alone or with LPS and IFNgamma. TG4-155 significantly reduces neurodegeneration in a mouse model of status epilepticus, induced by pilocarpine. It inhibits proliferation, invasion, and inflammatory cytokine expression in cancer cells treated with butaprost.
References: The Journal of Biological Chemisty288(13), 9293-9302 (2013).
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