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GLPG4471 is a selective and orally active IRAK4 inhibitor with an IC50 of 1.7 nM. It demonstrates potent inhibitory effects on cytokine secretion (TNFα and IFNα) in both cellular and whole blood phenotypic assays. Additionally, GLPG4471 shows significant activity in a collagen-induced arthritis mouse model and can be utilized for arthritis research.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | GLPG4471 is a selective and orally active IRAK4 inhibitor with an IC50 of 1.7 nM. It demonstrates potent inhibitory effects on cytokine secretion (TNFα and IFNα) in both cellular and whole blood phenotypic assays. Additionally, GLPG4471 shows significant activity in a collagen-induced arthritis mouse model and can be utilized for arthritis research. |
| Targets&IC50 | IRAK4:1.7 nM |
| In vitro | GLPG4471 effectively inhibits the secretion of TNFα and IFNα in human whole blood and peripheral blood mononuclear cells (PBMC) stimulated by CL097. The compound exhibits excellent metabolic stability in liver microsomes and hepatocytes from mice, rats, and humans, with predicted hepatic clearance rates ranging from low to moderate. |
| In vivo | GLPG4471, administered orally at doses of 3-30 mg/kg twice daily for 17 days, demonstrated dose-dependent activity in a collagen-induced arthritis mouse model. |
| Molecular Weight | 410.47 |
| Formula | C22H26N4O4 |
| Cas No. | 2499855-36-4 |
| Smiles | O=C(NC1=CC2=CC(=NN2C=C1OC)CCC(O)(C)C)C3=CC=CN(C3=O)C4CC4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
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
and mix thoroughly until a homogeneous solution is obtained.
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