All AbMole products are for research use only, cannot be used for human consumption.
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 |
|---|
| Zoniporide dihydrochloride
Zoniporide dihydrochloride (CP-597396 dihydrochloride) is a potent and selective inhibitor of highly water-soluble sodium hydrogen exchange type 1 (NHE-1). |
| Dimethylamiloride hydrochloride
Dimethylamiloride hydrochloride is a Na+/H+ exchanger NHE inhibitor with Ki values of 0.02, 0.25, and 14 μM for NHE1, NHE2, and NHE3, respectively. |
| NHE3-IN-1
NHE3-IN-1 is an inhibitor of sodium/proton exchanger 3 (NHE-3). |
| NHE3-IN-2
NHE3-IN-2 is a Na+/H+ exchanger 3 (NHE3) inhibitor. |
| Eniporide
Eniporide (EMD 96785) is a Na(+)/H(+) exchange (NHE) inhibitor. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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