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Tenapanor

Cat. No. M7572
Tenapanor Structure
Synonym:

AZD1722; RDX5791

Size Price Availability Quantity
5mg USD 220 In stock
10mg USD 340 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Rats
Formulation water
Dosages 10 ml/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 1145.05
Formula C50H66Cl4N₈O10S2
CAS Number 1234423-95-0
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

The effects of tenapanor on serum fibroblast growth factor 23 in patients receiving hemodialysis with hyperphosphatemia.
Block GA, et al. Nephrol Dial Transplant. 2018 Apr 3. PMID: 29617976.

A common NHE3 single-nucleotide polymorphism has normal function and sensitivity to regulatory ligands.
Yin J, et al. Am J Physiol Gastrointest Liver Physiol. 2017 Aug 1;313(2):G129-G137. PMID: 28495802.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tenapanor, AZD1722; RDX5791 supplier, Sodium Channel, inhibitors

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