Tenapanor

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tenapanor (AZD-1722;RDX5791) 是一种有效的选择性 Na+/H+ 交换器 3 (NHE3) 抑制剂，对人和大鼠 NHE3 的 IC50 分别为 5 和 10 nM。

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(In Vivo):Tenapanor (0.15, 0.5 mg/kg; p.o.) reduces passive paracellular phosphate absorption in rats.Tenapanor (0.15 mg/kg; p.o.; twice-daily for 11 consecutive days) increases the reduction in urinary phosphorus excretion in rats.

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Animal Model:Rats (intestinal loop model)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 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.

AZD-1722 | RDX5791

Membrane Transporter/Ion Channel

Sodium Channel

Sodium Channel

Cardiovascular Disease

Dyslipidemia

1234423-95-0

1145.044

C50H66Cl4N8O10S2

>98% (HPLC)

DMSO : 50 mg/mL43.67 mM;H2O : < 0.1 mg/mL

CN1CC(C2=C(C1)C(=CC(=C2)Cl)Cl)C3=CC(=CC=C3)S(=O)(=O)NCCOCCOCCNC(=O)NCCCCNC(=O)NCCOCCOCCNS(=O)(=O)C4=CC=CC(=C4)C5CN(CC6=C5C=C(C=C6Cl)Cl)C

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

(-20℃)

With Ice Pack

≥ 2 years