GLPG1205

Research use only, not for human use.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

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. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

GLPG1205 (0.5μM) completely inhibits the ZQ16-induced [Ca2+]i response in neutrophils. GLPG1205 (1μM; for 5min) completely blocks the ROS-response induced by the GPR84-agonist. GLPG1205 can potently antagonizes ZQ16-induced ROS with an IC50 value of 15nM in TNF-α primed neutrophils.

GLPG1250 (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.

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Cell Cycle/DNA Damage

GPR

GPR

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1445847-37-9

378.42

C22H22N2O4

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (660.64 mM; Ultrasonic )

O=c1nc(OC[C@@H]2COCCO2)cc2-c3ccc(cc3CCn12)C#CC1CC1

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(-20℃)

With Ice Pack

≥ 2 years