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

GKA50 

Cat. No.: HY-15671 Purity: >98.0%
Handling Instructions

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

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GKA50 Chemical Structure

GKA50 Chemical Structure

CAS No. : 851884-87-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 562 In-stock
Estimated Time of Arrival: December 31
1 mg USD 185 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 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 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 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 EC50values 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].

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].

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

464.51

Formula

C₂₆H₂₈N₂O₆

CAS No.

851884-87-2

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

Shipping

Room temperature in continental US; may vary elsewhere.

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

Purity: >98.0%

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Keywords:

GKA50GKA 50GKA-50GlucokinaseHexokinase IVHexokinase DglucoseinsulinMIN6highfatfedsecretionproliferationβ-cellsINS-1Inhibitorinhibitorinhibit

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Product name:
GKA50
Cat. No.:
HY-15671
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