Tenapanor
目录号: PL07615 纯度: ≥98%
CAS No. :1234423-95-0
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中文名称
Tenapanor
中文别名
Tenapanor;替那帕诺
英文名称
Tenapanor
英文别名
Tenapanor;AZD 1722;AZD-1722;RDX5791;RDX-5791;17-[[[3-[(4S)-6,8-Dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]-N-[2-[2-[2-[[[3-[(4S)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]ethoxy]ethoxy]ethyl]-8-oxo-12,15-dioxa-2,7,9-triazaheptadecanamide;AZD1722;Tenapanor free base;WYD79216A6;RDX 5791;Tenapanor [USAN:INN];Ibsrela;Tenapanor (USAN/INN);GTPL8449;BDBM381823;BCP24892;B
Cas No.
1234423-95-0
分子式
C50H66Cl4N8O10S2
分子量
1145.05
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Tenapanor (AZD1722) 是一种有效且具有口服活性的钠/氢交换异构体 3 (NHE3) (sodium/hydrogen exchanger isoform 3 (NHE3)) 抑制剂。Tenapanor 主要通过减少被动细胞旁磷酸盐通量来减少肠道对磷酸盐的吸收。Tenapanor 具有研究高磷血症的潜力。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
IC50: 5 nM (NHE3, human), 10 nM (NHE3, rat)
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
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
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 50 mg/mL (43.67 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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