产品描述: | Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research |
靶点: |
5-HT4 Receptor;5-HT2B Receptor;5-HTReceptor |
体内研究: |
马来酸替加色罗 (SDZ-HTF-919; 5 mg/kg/天; 腹腔注射; 连续五天) 在体内延迟肿瘤生长、减少转移、增加存活率并抑制 p-S6。 马来酸替加色罗 (0.1-2.0 mg/kg; 胃负荷前 15 分钟腹腔注射) 显着加速 db/db 小鼠的胃葡萄糖排空率,在 0.1mg/kg 的情况下将 30 分钟时留在胃中的膳食部分减少80% . |
参考文献: |
1. Wei Liu, et al. Repurposing the serotonin agonist Tegaserod as an anticancer agent in melanoma: molecular mechanisms and clinical implications. J Exp Clin Cancer Res. 2020 Feb 21;39(1):38. 2. M D Crowell, et al. The effects of tegaserod, a 5-HT receptor agonist, on gastric emptying in a murine model of diabetes mellitus. Neurogastroenterol Motil. 2005 Oct;17(5):738-43. 3. D T Beattie, et al. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Br J Pharmacol. 2004 Nov;143(5):549-60. |
溶解性: |
DMSO : ≥ 35 mg/mL (83.84 mM) H2O : 1 mg/mL (2.40 mM; Need ultrasonic) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.395 ml |
11.977 ml |
23.954 ml |
5 mM |
0.479 ml |
2.395 ml |
4.791 ml |
10 mM |
0.24 ml |
1.198 ml |
2.395 ml |
50 mM |
0.048 ml |
0.24 ml |
0.479 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。 |