GLPG4970 is a highly potent, selective dual SIK2/SIK3 inhibitor with IC50 of 0.3/0.7 nM respectively.
GLPG4970 shows weak inhibition of hERG channel with an IC50 of 29 μM as assessed using the MPC assay.
GLPG4970 dose-dependently inhibits TNFα release, with an IC50 of 3.6 nM and 8.1 nM, respectively in monocytes and macrophages stimulated with LPS, >4-fold more potent than GLPG3970.
GLPG4970 shows potent inhibition of TNFα production with an IC50 of 83 nM in human whole blood.
GLPG4970 (0.5-30 mg/kg, i.p.) reduced the release of TNFα in a dose-dependent mannerd in in vivo acute LPS challenge model in mice.
GLPG4970 (3, 10, and 30 mg/k, twice daily, orally) is active in reducing disease activity in a mouse DSS-induced model of colitis.
