1. Membrane Transporter/Ion Channel
  2. Sodium Channel

Tenapanor (Synonyms: AZD1722; RDX5791)

Cat. No.: HY-15991 Purity: 98.80%
Data Sheet SDS Handling Instructions

Tenapanor is an inhibitor of the Na+/H+ exchanger NHE3 with IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.

For research use only. We do not sell to patients.
Tenapanor Chemical Structure

Tenapanor Chemical Structure

CAS No. : 1234423-95-0

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10 mM * 1 mL in DMSO $315 In-stock
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5 mg $190 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Tenapanor is an inhibitor of the Na+/H+ exchanger NHE3 with IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.

IC50 & Target

IC50: 5 nM (NHE3, human), 10 nM (NHE3, rat)[1]

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[1].

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[1].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 0.8733 mL 4.3666 mL 8.7332 mL
5 mM 0.1747 mL 0.8733 mL 1.7466 mL
10 mM 0.0873 mL 0.4367 mL 0.8733 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

Tenapanor is prepared in water.

Rat: For urinary and fecal sodium assessments, 8-week-old Sprague-Dawley rats are randomized into groups before oral administration of vehicle or tenapanor (10ml/kg). After 16 to 24 hours, collected excreta are analyzed for electrolytes by ion chromatography. In normal rats, tenapanor doses ranges from 0.1 to 10 mg/kg. Higher doses within this range (1 to 10 mg/kg) are used to evaluate aldosterone levels and serum bicarbonate; lower doses (0.1 to 3 mg/kg) are used to evaluate urine electrolytes as well as other electrolytes[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

1145.05

Formula

C₅₀H₆₆Cl₄N₈O₁₀S₂

CAS No.

1234423-95-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 10 mM

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.80%

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Product Name:
Tenapanor
Cat. No.:
HY-15991
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