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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) 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)

Biological Activity

Tenapanor (AZD-1722;RDX5791) 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; displays no inhibitory activities against . human intestinal transporters NHE1 (SLC9A1), NHE2 (SLC9A2), TGR5 (GPBAR1), ASBT and Pit-1; 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, also reduces sodium and phosphorus absorption, protects against vascular calcification in rat model of CKD.

Dyslipidemia

Phase 3 Clinical

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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