AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
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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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 1442684-77-6 |
分子式 | C22H25N5O4 |
分子量 | 423.465 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 30 mg/mL(70.84 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |