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GSK199

Name: GSK199
Brand: TargetMol
SKU: T8861
Price: 59 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8861Cas No. 1549811-53-1

GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).

GSK199

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Purity: 99.44%

Catalog No. T8861Cas No. 1549811-53-1

GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$59	In Stock	In Stock
5 mg	$143	In Stock	In Stock
10 mg	$238	In Stock	In Stock
25 mg	$391	In Stock	In Stock
50 mg	$548	In Stock	In Stock
100 mg	$738	-	In Stock
200 mg	$993	-	In Stock
1 mL x 10 mM (in DMSO)	$167	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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Batch Information

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Purity:99.44%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).
Targets&IC50	PAD4:200 nM
In vivo	GSK199, in the murine collagen-induced arthritis model of rheumatoid arthritis. Mice were dosed daily from the time of collagen immunization with GSK199. Efficacy was assessed against a wide range of end-points, including clinical disease scores, joint histology and immunohistochemistry, serum and joint citrulline levels and quantification of synovial autoantibodies using a proteomic array containing joint peptides. Administration of GSK199 at 30 mg/kg led to significant effects on arthritis, assessed both by global clinical disease activity and by histological analyses of synovial inflammation, pannus formation and damage to cartilage and bone. In addition, significant decreases in complement C3 deposition in both synovium and cartilage were observed robustly with GSK199 at 10 mg/kg. Neither the total levels of citrulline measurable in joint and serum, nor levels of circulating collagen antibodies, were affected significantly by treatment with GSK199 at any dose level. In contrast, a subset of serum antibodies reactive against citrullinated and non-citrullinated joint peptides were reduced with GSK199 treatment.

Chemical Properties

Molecular Weight	468.98
Formula	C₂₄H₂₉ClN₆O₂
Cas No.	1549811-53-1
Smiles	Cl.CCn1c(cc2cccnc12)-c1nc2cc(cc(OC)c2n1C)C(=O)N1CCC[C@@H](N)C1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 11 mg/mL (23.46 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (2.13 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	2.1323 mL	10.6614 mL	21.3229 mL	106.6144 mL
5 mM	0.4265 mL	2.1323 mL	4.2646 mL	21.3229 mL
10 mM	0.2132 mL	1.0661 mL	2.1323 mL	10.6614 mL
20 mM	0.1066 mL	0.5331 mL	1.0661 mL	5.3307 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