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Tenapanor hydrochloride

Chemical Structure : Tenapanor hydrochloride

CAS No.: 1234365-97-9

Tenapanor hydrochloride (AZD-1722, RDX5791)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 1217.96
Formula C50H68Cl6N8O10S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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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