1. Metabolic Enzyme/Protease
  2. Glucokinase
  3. PSN-GK1

PSN-GK1 

Cat. No.: HY-U00411
Handling Instructions

PSN-GK1 is a potent glucokinase activator with an EC50 of 0.13 μM.

For research use only. We do not sell to patients.

PSN-GK1 Chemical Structure

PSN-GK1 Chemical Structure

CAS No. : 745051-61-0

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Description

PSN-GK1 is a potent glucokinase activator with an EC50 of 0.13 μM.

IC50 & Target

EC50: 0.13 μM[1]

In Vivo

PSN-GK1 exhibits an excellent pharmacokinetic profile, with high oral bioavailability, in the rat. PSN-GK1 can markedly reduce blood glucose which accompanied by a trend toward increased pancreatic insulin release. Separately, the antihyperglycemic actions of PSN-GK1 have been shown to be a result of both pancreatic and hepatic effects. In addition, PSN-GK1 engenders potent antihyperglycemic effects in diabetic rodents without causing hypoglycemia[1]. At 5 mM glucose, PSN-GK1 activates glucokinase (4.3-fold, EC50=130 nM), increases MIN6 insulin secretion (26-fold, EC50=267 nM) and 2-DG hepatocytic uptake (3-fold, EC50=1 μM). In C57Bl/6 mice, PSN-GK1 reduces blood glucose at 1 and 10 mg/kg (by mouth), but insulin is increased significantly at only the higher dose. In hyperinsulinaemic 10-mM glucose clamps, PSN-GK1 increases2-DG incorporation into liver glycogen sixfold, directly demonstrating liver effects[2].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Kinase Assay
[2]

Glucokinase activity is measured in a coupled reaction with glucose-6-phosphate dehydrogenase (G6PDH) by monitoring NADPH production at A340 in a plate reader after 15 min incubation at 24°C, in a final volume of 100 μL containing 25 mM HEPES pH 7.1, 25 mM KCl, 5 mM glucose, 1 mM ATP, 2 mM MgCl2, 1 mM DL-dithiothreitol, 1 mM NADP, 2.5 U/mL G6PDH, 0.4 μg GST-glucokinase. Ten dilutions of PSN-GK1 from 0.004 to 100 μM are tested, calculating and fitting fold changes in activity vs controls to sigmoidal curves using a four-parameter logistic model[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice[2]

C57Bl/6J mice Food is withdrawn 5 h before dosing, while water is available throughout. A blood sample is taken from the tail tip under local anaesthetic for glucose and insulin measurement. Thereafter, mice are weighed and dosed orally with PSN-GK1 (1 or 10 mg/kg) or vehicle. Blood samples are taken 15, 30, 60, 120 and 240 min after dosing, samples (20 μL) for glucose being taken into disposable micro-pipettes and added to 480 μL haemolysis reagent[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

438.54

Formula

C₂₀H₂₃FN₂O₄S₂

CAS No.

745051-61-0

SMILES

O=C(NC1=NC=C(F)S1)[[email protected]@H](C2=CC=C(S(=O)(C3CC3)=O)C=C2)CC4CCOCC4

Shipping

Room temperature in continental US; may vary elsewhere

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PSN-GK1

Cat. No.: HY-U00411