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。
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货号:
TK0357 -
规格:
- 1mg
- 5mg
- 10mg
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价格:
¥0.00
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。
| 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% |