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.

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GLPG1205 (0.5?μM) completely inhibits the ZQ16-induced [Ca]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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

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

In Vitro: DMSO : 250 mg/mL (660.64 mM; Need ultrasonic)配制储备液