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GLPG1205

Name: GLPG1205
Brand: TargetMol
SKU: T11411
Price: 84 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11411Cas No. 1445847-37-9

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

GLPG1205

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Purity: 99.94%

Catalog No. T11411Cas No. 1445847-37-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$84	In Stock	In Stock
5 mg	$207	In Stock	In Stock
10 mg	$353	In Stock	In Stock
25 mg	$598	-	In Stock
1 mL x 10 mM (in DMSO)	$226	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.94%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.
In vitro	When GLPG1205 is administered at a concentration of 1 μM for a duration of 5 minutes, it effectively prevents the generation of reactive oxygen species (ROS) triggered by the GPR84 agonist. In TNF-α primed neutrophils, GLPG1205 exhibits strong antagonistic activity against ZQ16-induced ROS, with an IC50 value of 15 nM. Additionally, at a concentration of 0.5 μM, GLPG1205 completely suppresses the ZQ16-induced increase in intracellular calcium levels ([Ca2+]i) in neutrophils[1].
In vivo	GLPG1250 inhibits the increase in MnSOD in lung bronchial epithelial cells and parenchymal macrophages, in the irradiation model. GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model. Oral administration of GLPG1250 (30mg/kg; twice daily for 2 weeks, starts from 7 days post-challenge) greatly reduces the Ashcroft score, in idiopathic pulmonary fibrosis model. Oral administration of GLPG1250 (30mg/kg; once daily starts from 18 weeks post irradition) significantly reduces college deposition in the mouse lung[1].

Chemical Properties

Molecular Weight	378.42
Formula	C₂₂H₂₂N₂O₄
Cas No.	1445847-37-9
Smiles	O=c1nc(OC[C@@H]2COCCO2)cc2-c3ccc(cc3CCn12)C#CC1CC1
Relative Density.	1.36 g/cm3 (Predicted)

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: 225 mg/mL (594.58 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 5 mg/mL (13.21 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	2.6426 mL	13.2128 mL	26.4257 mL	132.1283 mL
5 mM	0.5285 mL	2.6426 mL	5.2851 mL	26.4257 mL
10 mM	0.2643 mL	1.3213 mL	2.6426 mL	13.2128 mL
20 mM	0.1321 mL	0.6606 mL	1.3213 mL	6.6064 mL
50 mM	0.0529 mL	0.2643 mL	0.5285 mL	2.6426 mL
100 mM	0.0264 mL	0.1321 mL	0.2643 mL	1.3213 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