|3-((S)-6,8-二氯-2-甲基-1,2,3,4-四氢异喹啉-4-基)-N-(26-((3-((S)-6,8-二氯-2-甲基-1,2,3,4-四氢异喹啉-4-基)苯基)磺酰氨基)-10,17-二氧代-3,6,21,24-四氧杂-9,11,16,18-四氮杂二十六烷基)苯磺酰胺|CsnPharm

CAS No.: 1234423-95-0

Tenapanor Catalog No. CSN25305

Synonyms: AZD1722;RDX5791;Ibsrela

Tenapanor is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3, which plays a prominent role in sodium handling in the gastrointestinal tract and kidney, with IC50 values of 5 and 10 nM against human and rat NHE3, respectively.

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技术信息

生物活性

描述The management of sodium intake is clinically important in many disease states including heart failure, kidney disease, and hypertension. NHE3 (sodium-proton (Na⁺/H⁺) exchanger 3) makes the major contribution to intestinal sodium uptake. Tenapanor is a NHE3 inhibitor with IC₅₀ values of 5 and 10 nM against human and Rat NHE3, respectively. Upon administering single doses of tenapanor to rats, there were dose-dependent reductions in urinary sodium and increases in fecal sodium and luminal fluid mass, and these values were associated with increasing tenapanor concentration in the intestinal lumen. Stool form score increased with tenapanor dose from a baseline of 1.2 to 2.2 (0.3 mg/kg), 3.3 (1 mg/kg), and 4.5 (3 mg/kg). Further, the acute negative sodium balance observed in the absence of exogenous sodium diminished during prolonged feeding of a sodium-free diet with tenapanor administration. Furthermore, chronic administration of tenapanor to rats fed with standard chow (0.49% NaCl) caused a sustained reduction of urinary sodium and increase in fecal sodium, both of which normalized upon tenapanor withdrawal. Repeated administration of tenapanor at 1, 3, or 10 mg/kg per day increased day 3 to 4 plasma aldosterone concentrations. These data from normal rats support a mechanism of action in which tenapanor acts to reduce intestinal sodium uptake. In healthy human subjects, administration of 15 to 60 mg of tenapanor twice daily produced an increase in fecal sodium of 20 to 50 mmol/day and decreases of similar magnitude in urinary sodium^[1].
参考文献

[1] Spencer AG, Labonte ED, Rosenbaum DP, et al. Intestinal inhibition of the Na⁺/H⁺ exchanger 3 prevents cardiorenal damage in rats and inhibits Na⁺ uptake in humans. Sci Transl Med. 2014;6(227):227ra36

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.8733 mL
- 4.3666 mL
- 8.7333 mL
- 5 mM
- 0.1747 mL
- 0.8733 mL
- 1.7467 mL
- 10 mM
- 0.0873 mL
- 0.4367 mL
- 0.8733 mL

技术信息

CAS号

1234423-95-0

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C50H66Cl4N8O10S2

运输

蓝冰

分子量

1145.05

别名

AZD1722;RDX5791;Ibsrela

溶解度

DMSO	50.0 mg/mL (43.7 mM) warming
Water	Insoluble

动物实验配方

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