GKA50 quarterhydrate

Cat. No.: HY-15671A: FAQs
Data Sheet SDS COA Handling Instructions

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GKA50 quarterhydrate is a potent glucokinase activator (EC₅₀=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca²⁺-dependent modulator of insulin secretion. 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

Size	Price	Stock
1 mg	USD 185	Ask For Quote & Lead Time
5 mg	USD 550	Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of GKA50 quarterhydrate:

GKA50

Other Forms of GKA50 quarterhydrate:

GKA50 In-stock

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

MedChemExpress (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].

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

469.01

Formula

C₂₆H₂₈N₂O₆.1/4H₂O

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.[1/4].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 (98.08 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	2.1322 mL	10.6608 mL	21.3215 mL
5 mM	0.4264 mL	2.1322 mL	4.2643 mL
10 mM	0.2132 mL	1.0661 mL	2.1322 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: ≥98.0%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (253 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)

References

[1]. Coope GJ, et al. Predictive blood glucose lowering efficacy by Glucokinase activators in high fat fed female Zucker rats. Br J Pharmacol. 2006 Oct;149(3):328-35. [Content Brief]

[2]. McGlasson L, et al. The glucokinase activator GKA50 causes an increase in cell volume and activation of volume-regulated anion channels in rat pancreatic β-cells. Mol Cell Endocrinol. 2011 Aug 6;342(1-2):48-53. [Content Brief]

[3]. Johnson D, et al. Glucokinase activators: molecular tools for studying the physiology of insulin-secreting cells. Biochem Soc Trans. 2007;35(Pt 5):1208-1210. [Content Brief]

[4]. Johnson D, et al. Glucose-dependent modulation of insulin secretion and intracellular calcium ions by GKA50, a glucokinase activator. Diabetes. 2007;56(6):1694-1702. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1322 mL	10.6608 mL	21.3215 mL	53.3038 mL
	5 mM	0.4264 mL	2.1322 mL	4.2643 mL	10.6608 mL
	10 mM	0.2132 mL	1.0661 mL	2.1322 mL	5.3304 mL
	15 mM	0.1421 mL	0.7107 mL	1.4214 mL	3.5536 mL
	20 mM	0.1066 mL	0.5330 mL	1.0661 mL	2.6652 mL
	25 mM	0.0853 mL	0.4264 mL	0.8529 mL	2.1322 mL
	30 mM	0.0711 mL	0.3554 mL	0.7107 mL	1.7768 mL
	40 mM	0.0533 mL	0.2665 mL	0.5330 mL	1.3326 mL
	50 mM	0.0426 mL	0.2132 mL	0.4264 mL	1.0661 mL
	60 mM	0.0355 mL	0.1777 mL	0.3554 mL	0.8884 mL
	80 mM	0.0267 mL	0.1333 mL	0.2665 mL	0.6663 mL