
(E)-Elafibranor
CAS No. 575474-82-7
(E)-Elafibranor ( R112 | R112 | R 112 )
产品货号. M17545 CAS No. 575474-82-7
R112 是 Syk 激酶的 ATP 竞争性抑制剂。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥381 | 有现货 |
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5MG | ¥616 | 有现货 |
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10MG | ¥1021 | 有现货 |
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25MG | ¥1863 | 有现货 |
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50MG | ¥2803 | 有现货 |
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100MG | ¥4155 | 有现货 |
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500MG | ¥8748 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称(E)-Elafibranor
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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R112 是 Syk 激酶的 ATP 竞争性抑制剂。
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产品描述R112 is a Syk inhibitor. R112 inhibited degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC(50)] = 353 nmol/L) or basophils (histamine release, EC(50) = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC(50) = 490 nmol/L). R112 also blocked leukotriene C4 production and all proinflammatory cytokines tested. Subsequent molecular characterization indicated that R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor (inhibitory constant [K(i)] = 96 nmol/L).(In Vitro):R112 (0.001-10 μM; 1 h) dose-dependently inhibits anti-IgE-mediated tryptase release and histamine release with EC50s of 0.353 and 0.28 μM, inhibits histamine release by basophils stimulated with an EC50 value of 0.49 μM, inhibits secretion of LTC4, TNF-α, GM-CSF and IL-8 with EC50s of 0.115, 2.01, 1.58 and 1.75 μM, respectively.R112 (0-10 μM; 40 min) inhibits Syk target LAT (Y191) phosphorylation.
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体外实验R112 (0.001-10 μM; 1 h) dose-dependently inhibits anti-IgE-mediated tryptase release and histamine release with EC50s of 0.353 and 0.28 μM, inhibits histamine release by basophils stimulated with an EC50 value of 0.49 μM, inhibits secretion of LTC4, TNF-α, GM-CSF and IL-8 with EC50s of 0.115, 2.01, 1.58 and 1.75 μM, respectively.R112 (0-10 μM; 40 min) inhibits Syk target LAT (Y191) phosphorylation. Western Blot Analysis Cell Line:Human mast cells Concentration:0.4, 2 and 10 μM Incubation Time:40 min Result:Inhibited phosphorylation of the Syk target LAT (Y191) and also inhibited phosphorylation of Syk downstream events.
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体内实验——
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同义词R112 | R112 | R 112
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通路Others
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靶点Other Targets
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受体Syk
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研究领域Inflammation/Immunology
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适应症——
化学信息
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CAS Number575474-82-7
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分子量312.3
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分子式C16H13FN4O2
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纯度>98% (HPLC)
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溶解度DMSO : ≥ 41 mg/mL; 131.28 mM
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SMILESc1cc(cc(c1)O)Nc1nc(ncc1F)Nc1cc(ccc1)O
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化学全称3,3'-((5-fluoropyrimidine-2,4-diyl)bis(azanediyl))diphenol
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. Rossi AB, et al. J Allergy Clin Immunol. 2006 Sep;118(3):749-55.
产品手册




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