| Bioactivity | 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[1][2][3]. |
| Invitro | 马来酸替加色罗 (SDZ-HTF-919; 3-5 μM; 24-72 小时) 引起显着的时间和剂量依赖性细胞凋亡增加[1]。马来酸替加色罗 (3-5 μM; 8-18 小时) 降低 p-S6 ,p-p70 S6 (Thr421/Ser424)[1]。马来酸替加色罗 (0.1-3 μM; 24 小时) 有效抑制 5-HT 介导的大鼠离体胃底收缩 (pA2=8.3),与 5-HT2B 受体拮抗剂活性一致[3]。 Apoptosis Analysis[1] Cell Line: |
| Name | Tegaserod maleate |
| CAS | 189188-57-6 |
| Formula | C20H27N5O5 |
| Molar Mass | 417.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |