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T-5224

T-5224 是一种转录因子 c-Fos/activator protein (AP)-1 的选择性抑制剂,并具有抗炎作用。T-5224 可特异性地抑制 c-Fos/c-Jun 的DNA结合活性和 IL-1β 诱导的 Mmp-3、Mmp-13 和 Adamts-5 转录的上调。

  • 货号:
    TK0357
  • 规格:
    1mg
    5mg
    10mg
  • 价格:
    0.00

产品参数

CAS No.530141-72-1
生物活性T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
分子式C29H27NO8
分子量517.53
运输条件Room temperature in continental US; may vary elsewhere.
储存条件Powder, -20°C ,3 years
溶解性数据DMSO : 100 mg/mL (193.23 mM; Need ultrasonic)
体内研究Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS impartes appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduces the lethality (27%).G2 is observed in rat and monkey liver microsomes as a major metabolite of T-5224, suggesting that G2 is not a human-specific metabolite.T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice.
体外研究T-5224 inhibits in-vitro production of the mediators MMP-1, MMP-3, IL-6 and TNF-α by IL-1β-stimulated human synovial SW982 cells with the mean IC50 of about 10 μM.T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner.
纯度及产品资料98%