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In vitro: Tenapanor exhibits human and rat NHE3 with IC50 values of 5 and 10 nM, respectively. Human intestinal transporters NHE1, NHE2, TGR5, ASBT, and Pit-1 and the sodium-dependent phosphate transporter NaPiIIb are not inhibited by tenapanor at concentrations up to 10 to 30 μM.
In vivo: Tenapanor plays a prominent role in sodium handling in the gastrointestinal tract and kidney. It acts exclusively in the gastrointestinal tract to inhibit sodium uptake when administered orally to rats. Average plasma Cmax values of tenapanor in rats and humans are less than 1 ng/mL with negligible area under the curve at doses of up to 30mg/kg in rats, 10mg/kg in dogs, and 900 mg in humans. Dose-dependent reductions in urinary sodium and increases in fecal sodium and luminal fluid mass are observed upon administering single doses of tenapanor to rats. Chronic administration of tenapanor to rats fed with standard chow (0.49% NaCl) causes a sustained reduction of urinary sodium and increase in fecal sodium.
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Rats |
| Formulation | water |
| Dosages | 10 ml/kg |
| Administration | oral |
| Molecular Weight | 1145.05 |
| Formula | C50H66Cl4N₈O10S2 |
| CAS Number | 1234423-95-0 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Na+/H+ Exchanger (NHE) Products |
|---|
| KR-32568
KR-32568 is a sodium/hydrogen exchanger-1 (NHE-1) inhibitor with an IC50 value of 0.23 μM. |
| Cariporide
Cariporide is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. |
| EMD-87580
EMD-87580 is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. |
| FR183998 free base
FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively. |
| Tenapanor hydrochloride
Tenapanor (AZD1722) hydrochloride is a first-in-class, potent, orally active sodium/hydrogen exchange isomer 3 (NHE3) inhibitor that reduces intestinal phosphate absorption primarily by decreasing passive paracellular phosphate flux. Tenapanor hydrochloride reduces intestinal absorption of phosphate by reducing passive paracellular phosphate flux. Tenapanor hydrochloride is used in studies related to chronic renal insufficiency, hyperphosphatemia, constipation, and irritable bowel syndrome. |
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