[CAS NO. 1234423-95-0] Tenapanor

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PRODUCTS SPECIFICATIONS [1234423-95-0]

Catalog

HY-15991

Brand

MCE

CAS

1234423-95-0

DESCRIPTION [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

For research use only. We do not sell to patients.

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

In Vitro:

DMSO : 50 mg/mL ( 43.67 mM ; Need ultrasonic)

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (2.18 mM); Clear solution
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

* All of the co-solvents are available by MCE.

References

Synonyms

12,15-Dioxa-2,7,9-triazaheptadecanamide, 17-[[[3-[(4S)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]-N-[2-[2-[2-[[[3-[(4S)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]ethoxy]ethoxy]ethyl]-8-oxo-

17-[[[3-[(4S)-6,8-Dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]-N-[2-[2-[2-[[[3-[(4S)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]ethoxy]ethoxy]ethyl]-8-oxo-12,15-dioxa-2,7,9-triazaheptadecanamide

Tenapanor

Ibsrela

AZD 1722

AZD1722

AZD-1722