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| Cas No.: | 1442684-77-6 |
| Chemical Name: | AM 2394 |
| Synonyms: | AM-2394;AM2394;1-(6'-(2-hydroxy-2-methylpropoxy)-4-((5-methylpyridin-3-yl)oxy)-[3,3'-bipyridin]-6-yl)-3-methylurea;AM 2394;BCP18588;BDBM50533159;A16331;N-[6'-(2-Hydroxy-2-methylpropoxy)-4-[(5-methyl-3-pyridinyl)oxy][3,3'-bipyridin]-6-yl]-N'-methylurea;BA167876;1-[5-[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]-4-(5-methylpyridin-3-yl)oxypyridin-2-yl]-3-methylurea |
| SMILES: | O(C1C([H])=C([H])C(=C([H])N=1)C1=C([H])N=C(C([H])=C1OC1=C([H])N=C([H])C(C([H])([H])[H])=C1[H])N([H])C(N([H])C([H])([H])[H])=O)C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])O[H] |
| Formula: | C22H25N5O4 |
| M.Wt: | 423.4650 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM. |
| Target: | EC50: 60 nM (glucokinase)[1] |
| In Vivo: | AM-2394, a structurally distinct glucokinase activator that displays a robust reduction in plasma glucose during an oral glucose tolerance test (OGTT) in ob/ob mice at a dose of 3 mg/kg. AM-2394 increases the affinity of glucokinase (GK) for glucose by approximately 10-fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes. AM-2394 exhibits good-to-moderate cross species plasma clearance, volume of distribution, and oral bioavailability, allowing for further evaluation in animal models[1]. |
| Animal Administration: | Mice[1] In order to determine the effect of AM-2394 in an animal model of type 2 diabetes, it 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 each reduced glucose excursion, with maximal efficacy seen at 3 mg/kg. |
| References: | [1]. Dransfield PJ, 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. |
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