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.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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) | 30 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Glucokinase (GK) Products |
|---|
| AZD1092
AZD1092 is an orally active glucokinase (GK) activator with an EC50 value of 0.03 μM. |
| GKM-001
GKM-001 is a glucokinase (GK) activator that can be used in studies related to type 2 diabetes. |
| TMG-123
TMG-123 is a glucokinase (GK) activator that can be used in studies related to type 2 diabetes. |
| PB-201
PB-201 is a glucokinase activator (GKA) that can be used in studies related to type 2 diabetes. |
| MK-0941 free base
MK-0941 free base is an orally active glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
