AZD 7986

DPP-1抑制剂(IC50=3.9nM)；对DPP-1具有选择性，优于组织蛋白酶S、-L、-B、-K、-D、-E、-Z、-H和-G（所有IC50s=>20µM），以及>200种酶、受体、离子通道和转运蛋白；抑制人骨髓衍生的CD34+中性粒细胞祖细胞中中性粒细胞弹性蛋白酶、蛋白酶3和组织蛋白酶G的活化（IC50s分别为61.7、208.9和114.8nM）；在0.2、2和20mg/kg时抑制大鼠骨髓裂解物中中性粒细胞弹性蛋白酶和蛋白酶3的活化；抑制NET形成，提高存活率，并减少4T1小鼠乳腺癌模型中的肺转移数量。An inhibitor of DPP-1 (IC50 = 3.9 nM); selective for DPP-1 over cathepsins S, -L, -B, -K, -D, -E, -Z, -H, and -G (IC50s = >20 µM for all), as well as a panel of >200 enzymes, receptors, ion channels, and transporters; inhibits activation of neutrophil elastase, proteinase 3, and cathepsin G in human bone marrow-derived CD34+ neutrophil progenitor cells (IC50s = 61.7, 208.9, and 114.8 nM, respectively); inhibits activation of neutrophil elastase and proteinase 3 in rat bone marrow lysates at 0.2, 2, and 20 mg/kg; suppresses NET formation, increases survival, and reduces the number of lung metastases in a 4T1 murine mammary carcinoma model.分子式C23H24N4O4分子量420.5CN1C2=CC(C3=CC=C(C=C3)C[C@@H](C#N)NC([C@@H]4CNCCCO4)=O)=CC=C2OC1=O