S82509 |
Tenapanor |
源葉(MedMol) | 98% |
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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- 產(chǎn)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
- 靶點(diǎn): IC50: 5 nM (NHE3, human), 10 nM (NHE3, rat);SodiumChannel
- 體內(nèi)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.
- 參考文獻(xiàn):
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
- 保存條件: -20℃
- 配置溶液濃度參考:
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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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)