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S1P2和S1P4受体拮抗剂(IC50分别为17和237nM);对S1P2的选择性优于S1P1和S1P3(两者的IC50s=>10µM);在1和10µM时可逆转S1P诱导的HUVEC和SMC迁移抑制;在30mg/kg时可减轻盲肠结扎和穿刺诱发的脓毒症大鼠模型中的肺损伤、内皮功能障碍和肺水肿;抑制DES1(IC50=16.8µM)以及SK1和SK2(IC50s分别为25.1和4.3µM)An S1P2 and S1P4 receptor antagonist (IC50 = 17 and 237 nM, respectively); selective for S1P2 over S1P1 and S1P3 (IC50s = >10 µM for both); reverses S1P-induced inhibition of HUVEC and SMC migration at 1 and 10 µM; reverses S1P-induced inhibition of B16 murine melanoma cell migration; reduces lung injury, endothelial dysfunction, and pulmonary edema in a rat model of cecal ligation and puncture-induced sepsis at 30 mg/kg; inhibits DES1 (IC50 = 16.8 µM), as well as SK1 and SK2 (IC50s = 25.1 and 4.3 µM, respectively).
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