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GLPG1205

CAS No. 1445847-37-9

GLPG1205 ( —— )

产品货号. M32938 CAS No. 1445847-37-9

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。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥2005 有现货
10MG ¥3430 有现货
25MG ¥5366 有现货
500MG 获取报价 有现货
1G 获取报价 有现货
1 mL x 10 mM in DMSO ¥1672 有现货

生物学信息

  • 产品名称
    GLPG1205
  • 注意事项
    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
  • 产品简述
    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,可用于肺纤维化的相关研究。
  • 产品描述
    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.
  • 体外实验
    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.
  • 体内实验
    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.
  • 同义词
    ——
  • 通路
    Cell Cycle/DNA Damage
  • 靶点
    GPR
  • 受体
    GPR
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    1445847-37-9
  • 分子量
    378.42
  • 分子式
    C22H22N2O4
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO 中的溶解度 : 250 mg/mL (660.64 mM; 超声助溶 )
  • SMILES
    O=c1nc(OC[C@@H]2COCCO2)cc2-c3ccc(cc3CCn12)C#CC1CC1
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

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.?
产品手册
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