Enarodustat

泛HIF-PH抑制剂（对于HIF-PH1、-2和-3，Kis分别为16、61和101nM）；增加Hep3B细胞中的EPO水平（EC50=4.7µM）；增加对照大鼠的血浆EPO水平，以及3mg/kg剂量下5/6肾切除大鼠的血浆EPO和血红蛋白水平；降低链脲佐菌素诱发的糖尿病肾病大鼠和链脲佐菌素诱发的糖尿病肾病小鼠模型中的肾脏脂肪酸和氨基酸代谢，增加肾脏葡萄糖代谢。A pan HIF-PH inhibitor (Kis = 16, 61, and 101 nM for HIF-PH1, -2, and -3, respectively); increases EPO levels in Hep3B cells (EC50 = 4.7 µM); increases plasma EPO levels in control rats, as well as plasma EPO and hemoglobin levels in 5/6-nephrectomized rats at 3 mg/kg; decreases renal fatty acid and amino acid metabolism and increases renal glucose metabolism in streptozotocin-induced rat and alloxan-induced mouse models of diabetic nephropathy.分子式C17H16N4O4分子量340.3O=C(CNC(C1=C(C=C(CCC2=CC=CC=C2)N3N=CN=C13)O)=O)O