• 咨询热线
    客服服务热线 13671568941/15317326293
  • 在线咨询
  • 微信客服
    微信客服
  • 公众号
    扫码关注公众号

(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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥381 有现货
5MG ¥616 有现货
10MG ¥1021 有现货
25MG ¥1863 有现货
50MG ¥2803 有现货
100MG ¥4155 有现货
500MG ¥8748 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    (E)-Elafibranor
  • 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
    R112 是 Syk 激酶的 ATP 竞争性抑制剂。
  • 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.
  • 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.
  • 体内实验
    ——
  • 同义词
    R112 | R112 | R 112
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Syk
  • 研究领域
    Inflammation/Immunology
  • 适应症
    ——

化学信息

  • CAS Number
    575474-82-7
  • 分子量
    312.3
  • 分子式
    C16H13FN4O2
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO : ≥ 41 mg/mL; 131.28 mM
  • SMILES
    c1cc(cc(c1)O)Nc1nc(ncc1F)Nc1cc(ccc1)O
  • 化学全称
    3,3'-((5-fluoropyrimidine-2,4-diyl)bis(azanediyl))diphenol

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. Rossi AB, et al. J Allergy Clin Immunol. 2006 Sep;118(3):749-55.
产品手册
关联产品
  • Decarboxy Moxifloxac...

    脱羧莫西沙星是莫西沙星的脱羧化合物。

  • Chemerin-9 (149-157)...

    Chemerin-9 (149-157) TFA, the nonapeptide (149)YFPGQFAFS(157) (chemerin-9), corresponding to the C terminus of processed chemerin, retains most of the activity of the full-size protein, with regard to agonism toward the chemerinR.

  • SEP-0371845

    SEP-0371845 是一种生化产品。