EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes[1].
CCR4 antagonist 4 (compound 22) is a selective and potent antagonist of the CC chemokine receptor-4 (CCR4), with an IC50 of 0.02 μM. CCR4 antagonist 4 also blocks MDC-mediated chemotaxis (IC50: 0.007 μM) and Ca2+ mobilization (IC50: 0.003 μM). CCR4 antagonist 4 can be used for allergic inflammation research[1].