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

GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca2+-dependent modulator of insulin secretion. 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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 184 In-stock
Solution
10 mM * 1 mL in DMSO USD 184 In-stock
Solid
1 mg USD 70 In-stock
5 mg USD 180 In-stock
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Based on 1 publication(s) in Google Scholar

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GKA50 Related Antibodies

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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. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats[1][2][3][4].

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].

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

GKA50 Related Antibodies

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].

MedChemExpress (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

464.51

Formula

C26H28N2O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(NC(C2=CC(O[C@@H](C)CC3=CC=CC=C3)=CC(O[C@@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
Solvent & Solubility
In Vitro: 

DMSO : 46 mg/mL (99.03 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1528 mL 10.7640 mL 21.5281 mL
5 mM 0.4306 mL 2.1528 mL 4.3056 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.57%

COA (251 KB) HNMR (282 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1528 mL 10.7640 mL 21.5281 mL 53.8202 mL
5 mM 0.4306 mL 2.1528 mL 4.3056 mL 10.7640 mL
10 mM 0.2153 mL 1.0764 mL 2.1528 mL 5.3820 mL
15 mM 0.1435 mL 0.7176 mL 1.4352 mL 3.5880 mL
20 mM 0.1076 mL 0.5382 mL 1.0764 mL 2.6910 mL
25 mM 0.0861 mL 0.4306 mL 0.8611 mL 2.1528 mL
30 mM 0.0718 mL 0.3588 mL 0.7176 mL 1.7940 mL
40 mM 0.0538 mL 0.2691 mL 0.5382 mL 1.3455 mL
50 mM 0.0431 mL 0.2153 mL 0.4306 mL 1.0764 mL
60 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8970 mL
80 mM 0.0269 mL 0.1346 mL 0.2691 mL 0.6728 mL
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GKA50 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GKA50851884-87-2GKA 50GKA-50GlucokinaseHexokinase IVHexokinase DglucoseinsulinMIN6highfatfedsecretionproliferationβ-cellsINS-1Inhibitorinhibitorinhibit

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