GLPG1205

• 常用名: GLPG1205
• 英文名: GLPG1205
• CAS号: 1445847-37-9
• 分子量: 378.42
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₂H₂₂N₂O₄
• 熔点: N/A
• 闪点: N/A

GLPG1205用途

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。

GLPG1205名称

• 英文名: GLPG1205

GLPG1205生物活性

• 描述: 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。
• 相关类别:
  研究领域 >> 炎症/免疫
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> GPR84
• 体外研究: GLPG1205(0.5μM)完全抑制中性粒细胞ZQ16诱导的[Ca2+]i反应[1]。GLPG1205(1μM；5μM)完全阻断GPR84激动剂诱导的ROS反应[1]。GLPG1205对ZQ16诱导的ROS有较强的拮抗作用,其IC50值为15 nM。
• 体内研究: 在特发性肺纤维化模型中,GLPG1250(口服,30mg/kg,每日两次)从激发后7天开始持续2周,大大降低了Ashcroft评分[3]。GLPG1250(口服,30mg/kg,每日一次)从照射后18周开始,显著减少小鼠肺中的学院沉积。此外,在辐射模型中,GLPG1250抑制肺支气管上皮细胞和实质巨噬细胞中MnSOD的增加[3]。在小鼠IBD模型中,GLPG1205剂量依赖性地降低疾病活性、组织学活性、中性粒细胞内流和结肠MPO含量[4]。
• 参考文献:

  [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

GLPG1205物理化学性质

• 分子式: C₂₂H₂₂N₂O₄
• 分子量: 378.42
• InChIKey: IRBAWVGZNJIROV-SFHVURJKSA-N
• SMILES: O=c1nc(OCC2COCCO2)cc2n1CCc1cc(C#CC3CC3)ccc1-2

GLPG1205靶点实验

查看更多实验

实验名称：Selectivity ratio of IC50 for antagonist activity at GPR41 (unknown origin) expressed... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5159697

实验名称：Selectivity ratio of IC50 for antagonist activity at GPR40 (unknown origin) expressed... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5159696

实验名称：Inhibition of PDE4A (unknown origin) at 1 to 10 uM by fluorescence polarization based... 来源：ChEMBL 靶标：cAMP-specific 3',5'-cyclic phosphodiesterase 4A External Id：CHEMBL5159699

实验名称：Selectivity ratio of IC50 for antagonist activity at GPR119 (unknown origin) expresse... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5159698

实验名称：Antagonist activity at GPR84 expressed in mouse bone marrow cells assessed as reducti... 来源：ChEMBL 靶标：G-protein coupled receptor 84 External Id：CHEMBL5159693

实验名称：Selectivity ratio of IC50 for antagonist activity at GPR120 (unknown origin) expresse... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5159692

实验名称：Antagonist activity at GPR84 expressed in mouse bone marrow cells assessed as reducti... 来源：ChEMBL 靶标：G-protein coupled receptor 84 External Id：CHEMBL5159694

实验名称：Oral bioavailability in rat at 5 mg/kg 来源：ChEMBL 靶标：N/A External Id：CHEMBL5537435

实验名称：Half life in rat at 5 mg/kg, po 来源：ChEMBL 靶标：N/A External Id：CHEMBL5537434

实验名称：Clearance in rat at 1 mg/kg, iv 来源：ChEMBL 靶标：N/A External Id：CHEMBL5537433

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