GLPG1205

Modify Date: 2024-01-10 12:07:08

GLPG1205 Structure
GLPG1205 structure
Common Name GLPG1205
CAS Number 1445847-37-9 Molecular Weight 378.42
Density N/A Boiling Point N/A
Molecular Formula C22H22N2O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GLPG1205


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[1][2].

 Names

Name GLPG1205

 GLPG1205 Biological Activity

Description 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[1][2].
Related Catalog
In Vitro GLPG1205 (0.5 μM) completely inhibits the ZQ16-induced [Ca2+]i response in neutrophils[1]. GLPG1205 (1 μM; for 5 min) completely blocks the ROS-response induced by the GPR84-agonist[1]. GLPG1205 can potently antagonizes ZQ16-induced ROS with an IC50 value of 15 nM in TNF-α primed neutrophils[1].
In Vivo 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[3]. 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[3]. GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model[4].
References

[1]. Sundqvist M, et al. Similarities and differences between the responses induced in human phagocytes through activation of the medium chain fatty acid receptor GPR84 and the short chain fatty acid receptor FFA2R. Biochim Biophys Acta Mol Cell Res. 2018 May;1865(5):695-708.

[2]. F. Vanhoutte, et al. Human safety, pharmacokinetics and pharmacodynamics of the GPR84 antagonist GLPG1205, a potential new approach to treat IBD.

[3]. L.Saniere, et al. Characterization of GLPG1205 in Mouse Fibrosis Models: A Potent and Selective Antagonist of GPR84 for Treatment of Idiopathic Pulmonary Fibrosis. American Journal of Respiratory and Critical Care Medicine 2019;199:A1046

[4]. F. Vanhoutte, et al. Human safety, pharmacokinetics and pharmacodynamics

 Chemical & Physical Properties

Molecular Formula C22H22N2O4
Molecular Weight 378.42