MK-7246

一种CRTH2/DP2受体拮抗剂（Ki=2.5nM）；对CRTH2/DP2的选择性高于DP1、FP、IP和TP受体（Ki值分别为373nM、>25,100nM、>23,030nM和3,804nM），以及EP1-4（Ki值为7,668-23,330nM）；在表达人CRTH2/DP2的HEK293细胞中，抑制13,14-二氢-15-酮-PGD₂诱导的cAMP形成（IC₅₀=3nM）；抑制13,14-二氢-15-酮-PGD₂诱导的嗜酸性粒细胞形态变化（IC₅₀=2.2nM）以及在分离的人全血中嗜酸性粒细胞和嗜碱性粒细胞上CD11b的上调（IC₅₀分别为6.2nM和5.4nM）；在羊模型中，以1mg/kg剂量减少抗原诱导的晚期支气管收缩，并完全预防气道高反应性。A CRTH2/DP2 receptor antagonist (Ki = 2.5 nM); selective for CRTH2/DP2 over DP1, FP, IP, and TP receptors (Kis = 373, >25,100, >23,030, and 3,804 nM, respectively), as well as EP1-4 (Kis = 7,668-23,330 nM); inhibits 13,14-dihydro-15-keto-PGD2-induced inhibition of cAMP formation in HEK293 cells expressing human CRTH2/DP2 (IC50 = 3 nM); inhibits 13,14-dihydro-15-keto-PGD2-induced eosinophil shape change (IC50 = 2.2 nM) and CD11b upregulation on eosinophils and basophils in isolated human whole blood (IC50s = 6.2 and 5.4 nM, respectively); decreases antigen-induced late-phase bronchoconstriction and completely prevents airway hyperresponsiveness in sheep at 1 mg/kg.分子式C21H21FN2O4S分子量416.5OC(CC1=C2N(C[C@@H](CC2)N(C)S(=O)(C3=CC=C(C=C3)F)=O)C4=CC=CC=C41)=O