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AM-2394

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Chemical Structure| 1442684-77-6 同义名 : -
CAS号 : 1442684-77-6
货号 : A147455
分子式 : C22H25N5O4
纯度 : 99%+
分子量 : 423.465
MDL号 : MFCD30533320
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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:
生物活性
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
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

[1]Kohn TJ, Du X, et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med Chem Lett. 2016 Jun 1;7(7):666-70.

[2]Dransfield PJ, Pattaropong V, et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med Chem Lett. 2016 May 23;7(7):714-8.

[3]Dransfield PJ, Pattaropong V, et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med Chem Lett. 2016 May 23;7(7):714-8