GLPG2534 (C09-1134-739)

GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC 50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4 . GLPG2534 can be used for the research of inflammatory skin diseasesIn VitroGLPG2534 (2 h) inhibits IRAK4 with IC 50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 inhibits IL-1β–driven IL-6 release, with an IC 50 of 55 nM. GLPG2534 inhibits TNF-α–driven IL-6 release with an IC 50 of 6.6 μM. GLPG2534 (0.1-10 μM, 16 h) inhibits expression of S100A7, DEFB4A, CXCL8, TNF in Flagellin-stimulated keratinocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGLPG2534 (0.3-10 mg/kg, p.o.) Inhibits CL097-driven release of TNF-α in blood of mice . GLPG2534 (10 and 30 mg/kg, p.o., b.i.d. 5 days) attenuates inflammation in psoriasis-like mouse models . GLPG2534 (3-30 mg/kg, p.o., b.i.d. 5 days) attenuates the development of IL-33- and MC903-induced AD-like skin inflammation in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Psoriasis-like skin inflammation model, induced by IL-23 and IMQ Dosage: 10 and 30 mg/kg Administration: p.o., b.i.d. 5 days Result: Reduced IL-23-induced expression of pathogenic cytokines such as Il17a (79%), Il22 (49%), Il1b (97%), and defensin Lcn2 (69%).IC50& Target:hIRAK4 6.4 nM (IC 50 ) mIRAK4 3.5 nM (IC 50 ) IRAK1 179 nM (IC 50 ). Molecular Formula: C21H24N6O4. Molecular Weight: 424.45.