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GLPG3970

Name: GLPG3970
Brand: TargetMol
SKU: T73384
Price: 60 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T73384 Copy Product Info

Purity: 99.63%

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GLPG3970 (compound 88) is a small molecule inhibitor, a dual SIK2/SIK3 inhibitor (SIK2 IC50=7.8 nM, SIK3 IC50=3.8 nM) with selectivity over SIK1, oral activity, and cellular permeability. This compound possesses anti-inflammatory activity and can be used for research on autoimmune and inflammatory diseases.

Cas No. 2403733-82-2

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Pack Size	Price	USA Stock	Global Stock
1 mg	$60	In Stock	In Stock
5 mg	$139	In Stock	In Stock
10 mg	$198	In Stock	In Stock
25 mg	$396	In Stock	In Stock
50 mg	$596	In Stock	In Stock
100 mg	$865	-	In Stock
1 mL x 10 mM (in DMSO)	$158	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Batch Information

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Purity:99.63%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	GLPG3970 (compound 88) is a small molecule inhibitor, a dual SIK2/SIK3 inhibitor (SIK2 IC50=7.8 nM, SIK3 IC50=3.8 nM) with selectivity over SIK1, oral activity, and cellular permeability. This compound possesses anti-inflammatory activity and can be used for research on autoimmune and inflammatory diseases.
Targets & IC50	SIK3:3.8 nM, SIK2:7.8 nM, SIK1:282.8 nM
In vitro	Methods: ADP-Glo kinase assay was used to determine GLPG3970 activity against SIK kinases; NanoBRET assay in HEK293 cells was used to evaluate isoform selectivity; high-content imaging in U2OS cells was used to detect CRTC3 translocation; ELISA was used to measure cytokines in LPS-stimulated human primary monocytes, macrophages, and whole blood (pre-incubation for 1 hour, LPS stimulation for 2–20 hours). Results: GLPG3970 selectively inhibited SIK2/SIK3 (IC50 3.8–7.8 nM), induced CRTC3 nuclear translocation (EC50 1.7 μM), suppressed TNFα (IC50 67–1000 nM), and increased IL-10.[1]
In vivo	Methods: In a mouse model of IL-23-induced psoriatic epidermal hyperplasia, GLPG3970 (10 mg/kg; oral, twice daily for five consecutive days) was administered; in a mouse collagen antibody-induced arthritis (CAIA) model, GLPG3970 (60 mg/kg; oral, twice daily until sacrifice) was administered; and in a mouse T cell transfer model, GLPG3970 (10 mg/kg; oral, twice daily for seven consecutive days) was administered. Results: In the IL-23-induced psoriasis model, GLPG3970 significantly reduced ear thickness; in the CAIA model, GLPG3970 demonstrated favorable clinical efficacy; and in the T cell transfer model, GLPG3970 significantly reduced the disease activity index, outperforming the control group.[1]

Chemical Properties

Molecular Weight	504.5
Formula	C₂₅H₂₇F₃N₄O₄
Cas No.	2403733-82-2
Smiles	O=C1C=2C(OC)=CC(=CC2CCN1CC(F)(F)F)C3=CN=C4C=C(OCCN5CCOCC5)C=CN43

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 128.8 mg/mL (255.3 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.54 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	1.9822 mL	9.9108 mL	19.8216 mL	99.1080 mL
5 mM	0.3964 mL	1.9822 mL	3.9643 mL	19.8216 mL
10 mM	0.1982 mL	0.9911 mL	1.9822 mL	9.9108 mL
20 mM	0.0991 mL	0.4955 mL	0.9911 mL	4.9554 mL
50 mM	0.0396 mL	0.1982 mL	0.3964 mL	1.9822 mL
100 mM	0.0198 mL	0.0991 mL	0.1982 mL	0.9911 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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