| 产品描述： | Tenapanor (AZD1722) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor has the potential for the research of hyperphosphatemia |
| 靶点： |
IC50: 5 nM (NHE3, human), 10 nM (NHE3, rat);SodiumChannel |
| 体内研究： |
Tenapanor (0.15, 0.5 mg/kg; p.o.) reduces passive paracellular phosphate absorption in rats. Tenapanor (0.15 mg/kg; p.o.; twice-daily for 11 consecutive days) increases the reduction in urinary phosphorus excretion in rats. Animal Model: Rats (intestinal loop model) Dosage: 0.15, 0.5 mg/kg Administration: P.o. Result: Reduced passive paracellular phosphate absorption by reduced urinary phosphate and sodium excretion after the high-phosphate meal and increased sodium and phosphate delivery to the cecum. Animal Model: 8 weeks, 250 g male Sprague–Dawley rats Dosage: 0.15 mg/kg in combination with sevelamer (0%, 0.75%, 1.5%, and 3% (wt/wt)) Administration: Oral gavage; twice-daily for 11 consecutive days Result: Significantly augmented the reduction in urinary phosphorus excretion. |
| 参考文献： |
1. King AJ, et al. Inhibition of sodium/hydrogen exchanger 3 in the gastrointestinal tract by tenapanor reduces paracellular phosphate permeability. Sci Transl Med. 2018 Aug 29;10(456):eaam6474. 2. King AJ, et al. Combination treatment with tenapanor and sevelamer synergistically reduces urinary phosphorus excretion in rats. Am J Physiol Renal Physiol. 2021 Jan 1;320(1):F133-F144. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
0.873 ml |
4.367 ml |
8.733 ml |
| 5 mM |
0.175 ml |
0.873 ml |
1.747 ml |
| 10 mM |
0.087 ml |
0.437 ml |
0.873 ml |
| 50 mM |
0.017 ml |
0.087 ml |
0.175 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京