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RO-28-1675

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Catalog No. T16793Cas No. 300353-13-3
Alias Ro28-1675, Ro 28-1675

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.

RO-28-1675

RO-28-1675

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Purity: 98.13%
Catalog No. T16793Alias Ro28-1675, Ro 28-1675Cas No. 300353-13-3
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$53-In Stock
5 mg$125-In Stock
10 mg$196-In Stock
25 mg$396-In Stock
50 mg$649-In Stock
100 mg$987-In Stock
200 mg$1,380-In Stock
1 mL x 10 mM (in DMSO)$137-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.13%
ee:100%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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].
SynonymsRo28-1675, Ro 28-1675
Chemical Properties
Molecular Weight378.51
FormulaC18H22N2O3S2
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 & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 40 mg/mL (105.68 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.28 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6419 mL13.2097 mL26.4194 mL132.0969 mL
5 mM0.5284 mL2.6419 mL5.2839 mL26.4194 mL
10 mM0.2642 mL1.3210 mL2.6419 mL13.2097 mL
20 mM0.1321 mL0.6605 mL1.3210 mL6.6048 mL
50 mM0.0528 mL0.2642 mL0.5284 mL2.6419 mL
100 mM0.0264 mL0.1321 mL0.2642 mL1.3210 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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