Tegaserod 是一种口服有效的 5-羟色胺受体 4 (HTR4; 5-HT4R) 激动剂和 5-HT2B 受体拮抗剂。Tegaserod 对人重组 5-HT2A、5-HT2B 和 5-HT2C 受体的 pKis 分别为 7.5、8.4 和 7.0。Tegaserod 导致肿瘤细胞凋亡，减弱 PI3K/Akt/mTOR 信号传导并降低 S6 磷酸化。Tegaserod 具有抗肿瘤活性，同时具有用于肠易激综合征 (IBS) 研究的潜力。
| 生物活性 |
Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research. |
|---|---|
| 分子式 |
C16H23N5O
|
| 分子量 |
301.39
|
| CAS号 |
145158-71-0
|
| 中文名称 |
替加色罗
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Powder : -20°C 3 years 4°C 2 years In solvent : -80°C 6 months -20°C 1 month |
纯度： 98%
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