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GLPG1205

CAS No. : 1445847-37-9

MCE 站：GLPG1205

产品活性：GLPG1205 是有效的选择性，具有口服活性的 GPR84 (G 蛋白偶联受体)拮抗剂，表现出良好的 PK/PD 特征。GLPG1205 具有抗炎活性，可以用于治疗肺纤维化。

研究领域：GPCR/G Protein

作用靶点：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.

相关产品：Drug Repurposing Compound Library  |  Orally Active Compound Library  |  GPCR/G Protein Compound Library  |  Clinical Compound Library  |  Clinical Compound Library Plus  |  Drug Repurposing Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Setogepram sodium salt  |  GPR84 antagonist 8  |  6-OAU

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