生物活性 | |||
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描述 | Glucokinase (GK), a member of the hexokinase enzyme family, catalyzes the phosphorylation of glucose to glucose-6-phosphate in the presence of ATP. AM-2394 is a structurally distinct GK activator with an EC50 value of 60 nM, increasing the affinity of GK for glucose by approximately 10-fold. Importantly, AM-2394 exhibited good-to-moderate cross species plasma clearance, volume of distribution, and oral bioavailability. In an animal model of type 2 diabetes, AM-2394 was administered per os (PO) to male ob/ob mice 30 minutes prior to performing an oral glucose tolerance test (OGTT). Doses of 1, 3, 10, 30 mg/kg reduced glucose excursion, with maximal efficacy seen at 3 mg/kg[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.36mL 0.47mL 0.24mL |
11.81mL 2.36mL 1.18mL |
23.61mL 4.72mL 2.36mL |
参考文献 |
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