1. Metabolic Enzyme/Protease
  2. Glucokinase
  3. GKA50 quarterhydrate

GKA50 quarterhydrate 

Cat. No.: HY-15671A
Handling Instructions

GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 quarterhydrate stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.

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

GKA50 quarterhydrate Chemical Structure

GKA50 quarterhydrate Chemical Structure

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5 mg USD 520 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 quarterhydrate stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats[1][2].

In Vitro

GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC50 values ranging from 1 to 2 μM[2].
GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells[2].
GKA50 activates human glucokinase enzymatic activity with an EC50 of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC50 of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD[2].

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

Cell Proliferation Assay[2]

Cell Line: INS-1 cells (starved overnight with 3 μM glucose)
Concentration: 0.01-100 μM
Incubation Time: 24 hours
Result: Stimulated cell proliferation in a dose-dependent manner, with EC50 values ranging from 1 to 2 μM.
In Vivo

GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test[1].

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

Animal Model: High-fat-fed obese female Zucker (fa/fa) rats[1]
Dosage: 1, 3, 10, 30 mg/kg
Administration: Oral administration
Result: Significant percentage glucose lowering.
Molecular Weight

469.01

Formula

C₂₆H₂₈N₂O₆.¼H₂O

SMILES

O=C(C1=CC=C(NC(C2=CC(O[[email protected]@H](C)CC3=CC=CC=C3)=CC(O[[email protected]@H](C)COC)=C2)=O)N=C1)O.[1/4].O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
References
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Keywords:

GKA50 quarterhydrateGlucokinaseHexokinase IVHexokinase DglucoseinsulinMIN6highfatfedsecretionproliferationβ-cellsINS-1Inhibitorinhibitorinhibit

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Product Name:
GKA50 quarterhydrate
Cat. No.:
HY-15671A
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