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Tenapanor hydrochloride

Names

[ CAS No. ]:
1234365-97-9

[ Name ]:
Tenapanor hydrochloride

[Synonym ]:
tenapanor HCl
N,N'-(10,17-Dioxo-3,6,21,24-tetraoxa-9,11,16,18-tetraazahexacosane-1,26-diyl)bis{3-[(4S)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydro-4-isoquinolinyl]benzenesulfonamide} dihydrochloride
tenapanor hydrochloride
50605O2ZNS
RDX5791
AZD1722 hydrochloride
1,1'-(butane-1,4-diyl)bis{3-[2-(2-{2-[({3-[(4S)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl]phenyl}sulfonyl)amino]ethoxy}ethoxy)ethyl]urea} dihydrochloride
Benzenesulfonamide, N,N'-(10,17-dioxo-3,6,21,24-tetraoxa-9,11,16,18-tetraazahexacosane-1,26-diyl)bis[3-[(4S)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]-, hydrochloride (1:2)

Biological Activity

[Description]:

Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia[1][2].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel
Research Areas >> Metabolic Disease

[In Vivo]

Tenapanor hydrochloride (0.15, 0.5 mg/kg; p.o.) reduces passive paracellular phosphate absorption in rats[1]. Tenapanor hydrochloride (0.15 mg/kg; p.o.; twice-daily for 11 consecutive days) increases the reduction in urinary phosphorus excretion in rats[2]. Animal Model: Rats (intestinal loop model)[1] Dosage: 0.15, 0.5 mg/kg Administration: P.o. Result: Reduced passive paracellular phosphate absorption by reduced urinary phosphate and sodium excretion after the high-phosphate meal and increased sodium and phosphate delivery to the cecum. Animal Model: 8 weeks, 250 g male Sprague–Dawley rats[2] Dosage: 0.15 mg/kg in combination with sevelamer (0%, 0.75%, 1.5%, and 3% (wt/wt)) Administration: Oral gavage; twice-daily for 11 consecutive days Result: Significantly augmented the reduction in urinary phosphorus excretion.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C50H68Cl6N8O10S2

[ Molecular Weight ]:
1217.970

[ Exact Mass ]:
1214.263062

Related Compounds