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GSK256073

Name: GSK256073
Brand: TargetMol
SKU: T15432
Price: 67 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T15432Cas No. 862892-90-8

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

GSK256073

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Purity: 98.46%

Catalog No. T15432Cas No. 862892-90-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$67	In Stock	In Stock
2 mg	$98	In Stock	In Stock
5 mg	$163	In Stock	In Stock
10 mg	$263	In Stock	In Stock
25 mg	$463	In Stock	In Stock
50 mg	$682	In Stock	In Stock
100 mg	$969	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$178	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.46%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.
Targets&IC50	HCA2 (hydroxy-carboxylic acid receptor 2):pEC50: 7.5
In vitro	GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes. GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC50 value of 7.5 compared to 6.7 for niacin). In membranes prepared from Chinese hamster ovary cells expressing recombinant human HCA2, It has good activity versus the rat orthologue of HCA2 (pEC50 value of 6.9 compared to 6.4 for niacin) [2].
In vivo	GSK256073 (i.v.; 1-10 mg/kg) produces a dose-related decrease in NEFA, however, the enhanced in-ear temperature induced by 10 mg/kg i.v. GSK256073 is only 40% of that induced by 10 mg/kg i.v. niacin. GSK256073 (p.o.; 1, 30, and 100 mg/kg; in rat) displays that the fall in NEFA is of rapid onset and that the maximum is dose-related with inhibitions of 74, 81 and 88%, respectively. Although the duration was longer with a reduction of 91% still present 6 h post-dose at 10 mg/kg, triglycerides reduce is followed as a similar pattern [2].

Chemical Properties

Molecular Weight	256.69
Formula	C₁₀H₁₃ClN₄O₂
Cas No.	862892-90-8
Smiles	CCCCCn1c2nc(Cl)[nH]c2c(=O)[nH]c1=O
Relative Density.	1.373 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 16.67 mg/mL (64.94 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 1.5 mg/mL (5.84 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.8957 mL	19.4787 mL	38.9575 mL	194.7875 mL
5 mM	0.7791 mL	3.8957 mL	7.7915 mL	38.9575 mL
10 mM	0.3896 mL	1.9479 mL	3.8957 mL	19.4787 mL
20 mM	0.1948 mL	0.9739 mL	1.9479 mL	9.7394 mL
50 mM	0.0779 mL	0.3896 mL	0.7791 mL	3.8957 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

GSK256073

GSK256073

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