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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 |
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| 10MG | ￥3430 | 有现货 |
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| 25MG | ￥5366 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
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| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥1672 | 有现货 |
|
生物学信息
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产品名称GLPG1205
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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
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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。
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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.
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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.
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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.
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同义词——
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通路Cell Cycle/DNA Damage
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靶点GPR
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受体GPR
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研究领域——
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适应症——
化学信息
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CAS Number1445847-37-9
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分子量378.42
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分子式C22H22N2O4
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO 中的溶解度 : 250 mg/mL (660.64 mM; 超声助溶 )
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SMILESO=c1nc(OC[C@@H]2COCCO2)cc2-c3ccc(cc3CCn12)C#CC1CC1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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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.?
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