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GLPG4970

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Catalog No. T212381

GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis.

GLPG4970

GLPG4970

😃Good
Catalog No. T212381
GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis.
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
GLPG4970 is a potent, selective, orally active dual inhibitor of salt-inducible kinases 2 and 3 (SIK2/SIK3), with IC50 values of 0.3 nM and 0.7 nM, respectively. It exhibits weak inhibition of the hERG channel, with an IC50 value of 29 μM. GLPG4970 reduces the release of tumor necrosis factor α (TNFα) and increases the release of interleukin 10 (IL-10). This compound is applicable for research in inflammation and immunology, such as studies on colitis.
Targets&IC50
SIK2:0.3 nM
In vitro
GLPG4970 (Compound 8) inhibits various off-target kinases, with IC₅₀ values ranging from 4 nM to 292 nM. It induces nuclear translocation of CRTC3 in U2OS cells, with an EC₅₀ of 16 nM. In lipopolysaccharide-stimulated monocytes and macrophages, GLPG4970 dose-dependently inhibits TNFα release, with IC₅₀ values of 3.6 nM and 8.1 nM, respectively, and enhances IL-10 release.
In vivo
GLPG4970 (Compound 8) administered orally at doses of 0.5-30 mg/kg 15 minutes before LPS exposure reduces TNFα release and enhances IL-10 release in LPS-treated mice. Additionally, GLPG4970 at doses of 3-30 mg/kg, given orally twice daily, slows the progression of disease in a mouse model of colitis induced by dextran sulfate sodium (DSS).
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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