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GLPG1205

產品活性：GLPG1205 是有效的選擇性，具有口服活性的 GPR84 (G 蛋白偶聯受體)拮抗劑，表現出良好的 PK/PD 特征。GLPG1205 具有抗炎活性，可用于肺纖維化的相關研究。

研究領域：GPCR/G Protein

作用靶點：GPR84

In Vitro: GLPG1205 (0.5?μM) completely inhibits the ZQ16-induced [Ca²⁺]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 IC₅₀ value of 15?nM in TNF-α primed neutrophils.

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.
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.

相關產品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  Targeted Diversity Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  6-OAU  |  Fezagepras  |  GPR84 antagonist 8  |  ZQ-16  |  GPR84 antagonist 1  |  GPR84 antagonist 2  |  GPR84 antagonist 3

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