GLPG1205 (C09-1134-960)

GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.In VitroGLPG1205 (0.5 μM) completely inhibits the ZQ16-induced [Ca 2+ ]i response in neutrophils. GLPG1205 (1 μM; for 5 min) completely blocks the ROS-response induced by the GPR84-agonist. GLPG1205 can potently antagonizes ZQ16-induced ROS with an IC 50 value of 15 nM in TNF-α primed neutrophils. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGLPG1250 (orally adminstation; 30mg/kg; twice daily) for 2 weeks, starts from 7 days post-challenge,greatly reduces the Ashcroft score, in idiopathic pulmonary fibrosis model. GLPG1250 (orally adminstation; 30mg/kg; once daily) starts from 18 weeks post irradition, significantly reduces college deposition in the mouse lung. Additionlly, GLPG1250 inhibits the increase in MnSOD in lung bronchial epithelial cells and parenchymal macrophages, in the irradiation model. GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:Solid. Specification: 0.99 Molecular Formula: C22H22N2O4 Molecular Weight: 378.42 PubChem CID: 71616860 Isomeric SMILES: C1CC1C#CC2=CC3=C(C=C2)C4=CC(=NC(=O)N4CC3)OC[C@@H]5COCCO5