| Name | RO-28-1675 |
| Description | RO-28-1675 is a direct and selective glucokinase activator that indirectly affects the activity of the GK/GKRP (glucokinase regulatory protein) complex, with efficacy decreasing with increasing glucose concentration, and can be used in studies related to insulin secretion and type 2 diabetes. |
| In vitro | In experiments with rat islet (Langerhans islet) cells and primary rat hepatocytes, RO-28-1675 showed an effect on the nuclear-cytoplasmic transport of glucokinase (GCK) in hepatocytes. Additionally, RO-28-1675 (3 μM) was able to lower the glucose concentration threshold required to stimulate insulin secretion. This suggests that RO-28-1675 not only regulates the subcellular localization of GCK but also enhances the glucose sensitivity of islet cells, thereby promoting insulin secretion [1]. |
| In vivo | In a diabetic mouse model with a Gck gene mutation, oral administration of RO-28-1675 (50 mg/kg) induced hypoglycemia in wild-type mice [2]. Pharmacokinetic studies indicated that RO-28-1675 has excellent absorption properties, with an oral bioavailability of 92.8% in mice. After a single dose of 10 mg/kg, the peak plasma concentration (Cmax) reached 1140 μg/mL [3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.28 mM), Sonication is recommended.
DMSO : 40 mg/mL (105.68 mM), Sonication is recommended.
|
| Keywords | RO-28-1675 | RO281675 | RO 28 1675 |
| Inhibitors Related | Gcase activator 2 | ARRY-403 | ML251 | PFK-015 | PFKFB3-IN-2 | D-(-)-3-Phosphoglyceric acid disodium | Oxfendazole | AZ PFKFB3 26 | AMG-1694 | PFK-158 | Dorzagliatin | PF-04937319 |
| Related Compound Libraries | Glycolysis Compound Library | Bioactive Compound Library | ReFRAME Related Library | Kinase Inhibitor Library | Post-Translational Modification Compound Library | Bioactive Compounds Library Max |
United States
