| 产品描述: | Tropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor |
| 靶点: |
5-HT3 receptor:5.3 nM(Ki);α7 nAChR:6.9 nM(Ki);5-HTReceptor;AChR |
| 体内研究: |
Tropisetron could ameliorate the ischemic brain injury via decreasing myeloperoxidase activity and TNF-α level. Tropisetron elicits anti-inflammatory effects in experimental model of cisplatin-induced nephrotoxicity and these effects were completely 5-HT3-receptor-independent |
| 细胞实验: |
Cell lines: Jurkat cells Concentrations: 10, 25, 50 μg/ml Incubation Time: 30 min Method: Jurkat cells (1 × 106 cells/ml) were stimulated with either TNFα (2 ng/ml) or PMA (20 ng/ml) plus ionomycin (0.5 ug/ml) for p65, JNK, ERK1 + 2, p38 and IκBα proteins in the presence or absence of tropisetron. Cells were then washed with PBS and proteins extracted in 50 μl of lysis buffer containing 0.5% NP-40. Protein concentration was determined by the Bradford assay and 30 μg of proteins were boiled in Laemmli buffer and electrophoresed in 10% SDS/polyacrylamide gels. |
| 动物实验: |
Animal Models: Male albino mice Dosages: 3 mg/kg Administration: i.p. |
| 参考文献: |
1. Macor JE, et al. Bioorg Med Chem Lett. 2001, 11(3):319-21. 2. Vega Lde L, et al. Biochem Pharmacol. 2005, 70(3):369-80. 3. Zirak MR, et al. Eur J Pharmacol. 2014, 738:222-9. |
| 溶解性: |
Soluble in DMSO、H2O |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.517 ml |
17.584 ml |
35.168 ml |
| 5 mM |
0.703 ml |
3.517 ml |
7.034 ml |
| 10 mM |
0.352 ml |
1.758 ml |
3.517 ml |
| 50 mM |
0.07 ml |
0.352 ml |
0.703 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。 |