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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-Tenapanor hydrochloride
Tenapanor hydrochloride

Chemical Structure : Tenapanor hydrochloride

CAS No.: 1234365-97-9

Tenapanor hydrochloride (AZD-1722, RDX5791)

货号: PC-63146Not For Human Use, Lab Use Only.

Tenapanor (AZD-1722, RDX5791) hydrochloride is a potent, selective inhibitor of the Na+/H+ exchanger 3 (NHE3) with IC50 of 5 and 10 nM for human and rat NHE3, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tenapanor (AZD-1722, RDX5791) hydrochloride is a potent, selective inhibitor of the Na+/H+ exchanger 3 (NHE3) with IC50 of 5 and 10 nM for human and rat NHE3, respectively.
Tenapanor displays no inhibitory activities against . human intestinal transporters NHE1 (SLC9A1), NHE2 (SLC9A2), TGR5 (GPBAR1), ASBT and Pit-1。
Tenapanor inhibits sodium uptake acted exclusively in the gastrointestinal tract in vivo, reduces extracellular fluid volume, left ventricular hypertrophy, albuminuria, and blood pressure in salt-fed nephrectomized rats。
Tenapanor also reduces sodium and phosphorus absorption, protects against vascular calcification in rat model of CKD.

物理化学性质&存储条件

分子量 1217.96
分子式 C50H68Cl6N8O10S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-((S)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)-N-(26-((3-((S)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)phenyl)sulfonamido)-10,17-dioxo-3,6,21,24-tetraoxa-9,11,16,18-tetraazahexacosyl)benzenesulfonamide dihydrochloride

参考文献

1. Spencer AG, et al. Sci Transl Med. 2014 Mar 12;6(227):227ra36.

2. Labonté ED, et al. J Am Soc Nephrol. 2015 May;26(5):1138-49.

3. Zielińska M, et al. Expert Opin Investig Drugs. 2015;24(8):1093-9.

4. Block GA, et al. Clin J Am Soc Nephrol. 2016 Sep 7;11(9):1597-605.

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