KRP 203

一种S1P1激动剂；选择性地诱导表达小鼠S1P1的CHO-K1细胞中的钙动员，而非小鼠S1P3和S1P4（EC50s分别为0.84、>1,000和9.61nM）；在IL10-/-小鼠结肠炎模型中，以0.3mg/kg的剂量预防消瘦综合征的发展、减少腹泻和结肠炎症细胞浸润并增加结肠长度；在次要组织相容性复合体-不同心脏移植的大鼠模型中，抑制炎症细胞浸润并延长同种异体移植存活率An S1P1 agonist; selectively induces calcium mobilization in CHO-K1 cells expressing mouse S1P1 over mouse S1P3 and S1P4 (EC50s = 0.84, >1,000, and 9.61 nM, respectively); prevents the development of wasting syndrome, decreases diarrhea and colonic inflammatory cell infiltration, and increases colon length in an IL10-/- mouse model of colitis at 0.3 mg/kg; inhibits inflammatory cell infiltration and prolongs allograft survival in a rat model of minor histocompatibility complex-disparate heart transplantation.