GLPG1205

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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，可用于肺纤维化的相关研究。

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 中的溶解度 : 250 mg/mL (660.64 mM; 超声助溶 )

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

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(-20℃)

With Ice Pack

≥ 2 years