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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.
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| Animal models | Mice |
| Formulation | |
| Dosages | 3 mg/kg |
| Administration | oral |
| Molecular Weight | 423.47 |
| Formula | C22H25N5O4 |
| CAS Number | 1442684-77-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Glucokinase (GK) Products |
|---|
| LY2608204
LY2608204 activates glucokinase (GK) with EC50 of 42 nM. |
| Dorzagliatin
Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a glucokinase (GK) activator, which improves glycaemic control and pancreatic β-cell function for type 2 diabetes. |
| AZD1656
AZD1656 is a potent, selective and orally active glucokinase (GK) activator, with an EC50 of 60 nM. |
| Cadisegliatin (TTP-399)
Cadisegliatin (TTP-399) is a potential, orally active liver-selective glucokinase (GK) activator. Cadisegliatin has antihyperglycaemic activity. Cadisegliatin can be used for the research of type 2 diabetes. |
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