S82509 |
Tenapanor |
源叶(MedMol) | 98% |
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- 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: -20℃
- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)