| 產(chǎn)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 |
| 靶點： |
5-HT4?Receptor;5-HT2B Receptor;5-HTReceptor |
| 體內(nèi)研究： |
馬來酸替加色羅 (SDZ-HTF-919; 5 mg/kg/天; 腹腔注射; 連續(xù)五天) 在體內(nèi)延遲腫瘤生長、減少轉(zhuǎn)移、增加存活率并抑制 p-S6。 馬來酸替加色羅 (0.1-2.0 mg/kg; 胃負(fù)荷前 15 分鐘腹腔注射) 顯著加速 db/db 小鼠的胃葡萄糖排空率，在 0.1mg/kg 的情況下將 30 分鐘時留在胃中的膳食部分減少80% . |
| 參考文獻： |
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) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京