CP 91,149

LGPa、MGPa和MGPb的抑制剂（在葡萄糖存在下，IC50s分别为0.13、0.2和0.3μM）；抑制原代人肝细胞中胰高血糖素刺激的糖原分解（IC50=2.1μM），并在5mM葡萄糖存在下以2.5μM的浓度增加大鼠肝细胞中的糖原合成；抑制脑GP（IC50=0.5μM）和表达内源性脑GP的A549NSCLC细胞的糖原积累和增殖（30μM）；在给药后3小时内降低糖尿病ob/ob小鼠的血糖水平，而不会产生低血糖，但对血糖正常的非糖尿病小鼠无影响（25mg/kg，口服）。An inhibitor of LGPa, MGPa, and MGPb (IC50s = 0.13, 0.2, and 0.3 μM, respectively, in the presence of glucose); inhibits glucagon-stimulated glycogenolysis in primary human hepatocytes (IC50 = 2.1 μM) and increases glycogen synthesis in rat hepatocytes at a concentration of 2.5 μM in the presence of 5 mM glucose; inhibits brain GP (IC50 = 0.5 μM) and glycogen accumulation and proliferation of A549 NSCLC cells that express endogenous brain GP (30 μM); lowers plasma glucose level in diabetic ob/ob mice within 3 hours of administration without producing hypoglycemia, but has no effect on normoglycemic, non-diabetic mice (25 mg/kg, p.o.).