| 产品描述: | Rafutrombopag (tautomerism) (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR‐expressing cells, including 32D‐ MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease. |
| 体外研究: |
Rafutrombopag (0.01-1000 nM, 0-7 days) 可刺激细胞内 TPO 信号通路,并以 TPOR 依赖的方式促进 32D-MPL (EC50 = 0.4 nM) 和 BaF3/h TPOP (EC50 = 1.2 nM) 细胞增殖。 Rafutrombopag (0.01-10 μM, 0-10 days) 可促进人脐带血来源的 CD34+ 细胞的增殖 (EC50 = 2.3 nM) 和分化。 Rafutrombopag (0-3 μM, 24-72 h) 可使 32D-MPL 细胞和大鼠心肌细胞的细胞周期进程正常化,并防止细胞凋亡。 Rafutrombopag (0.01-1000 nM, 30 min-72 h) 可与 TPOR 特异性结合,并与 rhTPO 产生叠加的激动效应。 Rafutrombopag (0.3-3 μM, 12 h) 可通过提高人脐血单个核细胞的活力和增加旁分泌因子的分泌,增强人脐血单个核细胞在氧自由基应激期间受损心肌细胞存活率的有益作用。 Rafutrombopag (3-30 μM) 具有抗炎活性,可显著减少 LPS 刺激下的巨噬细胞 RAW264.7 细胞中 NO 和 TNF-a 的产生。 |
| 体内研究: |
Rafutrombopag (18 mg/kg, p.o., 单剂量) 在小鼠中 3 小时时血浆浓度达到峰值 687 ng/mL,24 小时时降至 4.5 ng/mL,STAT3、STAT5 和 ERK1/2 的磷酸化在 3 小时时首次检测到,在 6-12 小时达到峰值,并持续至 24 小时。 Rafutrombopag (18 mg/kg, p.o., 每日一次,连续 12 天) 以时间依赖性方式显著刺激小鼠中空纤维内 32D-MPL 细胞的增殖并防止其凋亡。 |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.181 ml |
10.906 ml |
21.812 ml |
| 5 mM |
0.436 ml |
2.181 ml |
4.362 ml |
| 10 mM |
0.218 ml |
1.091 ml |
2.181 ml |
| 50 mM |
0.044 ml |
0.218 ml |
0.436 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |