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[CAS NO. 1234423-95-0] Tenapanor
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15991 |
| Brand: | MCE |
| CAS: | 1234423-95-0 |
Overview
| MDL | MFCD28386333 |
|---|---|
| Molecular Weight | 1145.05 |
| Molecular Formula | C50H66Cl4N8O10S2 |
| SMILES | O=C(NCCOCCOCCNS(=O)(C1=CC=CC([C@@H]2CN(C)CC3=C2C=C(Cl)C=C3Cl)=C1)=O)NCCCCNC(NCCOCCOCCNS(=O)(C4=CC=CC([C@@H]5CN(C)CC6=C5C=C(Cl)C=C6Cl)=C4)=O)=O |
4 Publications Citing Use of MCE
Summary
Tenapanor (AZD1722) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor has the potential for the research of hyperphosphatemia [1] [2] .
IC50 & Target
IC50: 5 nM (NHE3, human), 10 nM (NHE3, rat) [1]
In Vivo
Tenapanor (0.15, 0.5 mg/kg; p.o.) reduces passive paracellular phosphate absorption in rats
[1]
.
Tenapanor (0.15 mg/kg; p.o.; twice-daily for 11 consecutive days) increases the reduction in urinary phosphorus excretion in rats
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Rats (intestinal loop model) [1] |
| 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 [2] |
| 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. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02727751 | Ardelyx |
Constipation Predominant Irritable Bowel Syndrome
|
March 2016 | Phase 3 |
| NCT02249936 | Ardelyx|AstraZeneca |
Healthy
|
February 2013 | Phase 1 |
| NCT02063386 | Ardelyx |
Healthy Volunteers
|
April 2014 | Phase 1 |
| NCT03427125 | Ardelyx |
Hyperphosphatemia
|
January 8, 2018 | Phase 3 |
| NCT02621892 | Ardelyx |
Constipation Predominant Irritable Bowel Syndrome
|
October 2015 | Phase 3 |
| NCT01923428 | Ardelyx |
Constipation Predominant Irritable Bowel Syndrome
|
August 2013 | Phase 2|Phase 3 |
| NCT02226783 | Ardelyx |
Healthy Volunteers Food Interaction Study
|
March 2013 | Phase 1 |
| NCT01847092 | Ardelyx|AstraZeneca |
Chronic Kidney Disease|Type 2 Diabetes Mellitus
|
May 2013 | Phase 2 |
| NCT01764854 | Ardelyx|AstraZeneca |
End Stage Renal Disease|Chronic Kidney Disease Stage 5|ESRD
|
January 2013 | Phase 2 |
| NCT04549597 | Ardelyx |
Chronic Kidney Disease Requiring Chronic Dialysis|Hyperphosphatemia
|
November 20, 2020 | Phase 4 |
| NCT02675998 | Ardelyx |
Hyperphosphatemia
|
January 2016 | Phase 3 |
| NCT03824587 | Ardelyx |
Hyperphosphatemia
|
February 28, 2019 | Phase 2|Phase 3 |
| NCT01340053 | Ardelyx |
Constipation Predominant Irritable Bowel Syndrome
|
May 2011 | Phase 2 |
| NCT02176252 | Ardelyx|AstraZeneca |
Healthy Volunteer
|
July 2013 | Phase 1 |
| NCT03988920 | Ardelyx |
Hyperphosphatemia|End Stage Renal Disease
|
June 15, 2019 | Phase 4 |
| NCT02346890 | Ardelyx|AstraZeneca |
Healthy
|
April 2013 | Phase 1 |
| NCT02140268 | Ardelyx |
Healthy Volunteers
|
May 2014 | Phase 1 |
| NCT02796131 | Ardelyx |
Healthy
|
July 2011 | Phase 1 |
| NCT02081534 | Ardelyx |
Hyperphosphatemia
|
March 2014 | Phase 2 |
| NCT02686138 | Ardelyx |
Constipation Predominant Irritable Bowel Syndrome
|
December 2015 | Phase 3 |
| NCT02140281 | Ardelyx |
Healthy Volunteers
|
May 2014 | Phase 1 |
| NCT02819687 | Ardelyx |
Healthy
|
November 2010 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 43.67 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (2.18 mM); Suspended solution; Need ultrasonic
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (2.18 mM); Clear solution
-
4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (2.18 mM); Suspended solution; Need ultrasonic
References
- [1] King AJ, et al. Inhibition of sodium/hydrogen exchanger 3 in the gastrointestinal tract by tenapanor reduces paracellular phosphate permeability. Sci Transl Med. 2018 Aug 29;10(456):eaam6474.
- [2] King AJ, et al. Combination treatment with tenapanor and sevelamer synergistically reduces urinary phosphorus excretion in rats. Am J Physiol Renal Physiol. 2021 Jan 1;320(1):F133-F144.
Synonyms
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