GKA 50 is a potent glucokinase activator (EC50 = 33 nM). Significantly reduces plasma glucose levels in diabetic rats; stimulates insulin release from mouse islets of Langerhans.
| Molecular Weight | 464.51 |
| Formula | C26H28N2O6 |
| CAS Number | 851884-87-2 |
| Solubility (25°C) | DMSO 46.45 mg/mL |
| 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. |
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