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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $91 | In Stock | |
5 mg | $223 | In Stock | |
10 mg | $385 | In Stock | |
25 mg | $633 | In Stock | |
50 mg | $892 | In Stock | |
100 mg | $1,180 | In Stock | |
200 mg | $1,620 | In Stock | |
1 mL x 10 mM (in DMSO) | $245 | In Stock |
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. |
Targets&IC50 | GK:54 nM (EC50) |
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]. |
Alias | Ro28-1675, Ro 28-1675 |
Molecular Weight | 378.51 |
Formula | C18H22N2O3S2 |
Cas No. | 300353-13-3 |
Smiles | [C@@H](C(NC1=NC=CS1)=O)(CC2CCCC2)C3=CC=C(S(C)(=O)=O)C=C3 |
Relative Density. | 1.306 g/cm3 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (105.68 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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