Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a glucokinase (GK) activator, which improves glycaemic control and pancreatic β-cell function for type 2 diabetes.
| Molecular Weight | 462.93 |
| Formula | C22H27ClN4O5 |
| CAS Number | 1191995-00-2 |
| Solubility (25°C) | DMSO 83 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 |
|---|
| 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. |
| AMG-1694
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals. |
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