Tenapanor free base
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MedKoo CAT#: 329611

CAS#: 1234423-95-0 (free base)

Description: Tenapanor, also known as AZD-1722 and RDX 5791, is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3, which plays a prominent role in sodium handling in the gastrointestinal tract and kidney. Tenapanor possesses an excellent preclinical safety profile and, as of now, there are no serious concerns about its side effects. Tenapanor is currently in clinical trials.


Chemical Structure

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Tenapanor free base
CAS# 1234423-95-0 (free base)

Theoretical Analysis

MedKoo Cat#: 329611
Name: Tenapanor free base
CAS#: 1234423-95-0 (free base)
Chemical Formula: C50H66Cl4N8O10S2
Exact Mass: 1,142.31
Molecular Weight: 1,145.044
Elemental Analysis: C, 52.45; H, 5.81; Cl, 12.38; N, 9.79; O, 13.97; S, 5.60

Price and Availability

Size Price Availability Quantity
50mg USD 550 2 Weeks
100mg USD 950 2 Weeks
200mg USD 1650 2 Weeks
500mg USD 3250 2 Weeks
1g USD 4850 2 weeks
2g USD 7450 2 weeks
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Related CAS #: 1234423-95-0 (free base)   1234365-97-9 (2HCl)  

Synonym: AZD-1722; AZD 1722; AZD1722; RDX 5791; RDX-5791; RDX5791; Tenapanor free base; Ibsrela.

IUPAC/Chemical Name: 3-((S)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)-N-(26-((3-((S)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)phenyl)sulfonamido)-10,17-dioxo-3,6,21,24-tetraoxa-9,11,16,18-tetraazahexacosyl)benzenesulfonamide

InChi Key: DNHPDWGIXIMXSA-CXNSMIOJSA-N

InChi Code: InChI=1S/C50H66Cl4N8O10S2/c1-61-31-43(41-27-37(51)29-47(53)45(41)33-61)35-7-5-9-39(25-35)73(65,66)59-15-19-71-23-21-69-17-13-57-49(63)55-11-3-4-12-56-50(64)58-14-18-70-22-24-72-20-16-60-74(67,68)40-10-6-8-36(26-40)44-32-62(2)34-46-42(44)28-38(52)30-48(46)54/h5-10,25-30,43-44,59-60H,3-4,11-24,31-34H2,1-2H3,(H2,55,57,63)(H2,56,58,64)/t43-,44-/m0/s1

SMILES Code: O=S(C1=CC=CC([C@@H]2CN(C)CC3=C2C=C(Cl)C=C3Cl)=C1)(NCCOCCOCCNC(NCCCCNC(NCCOCCOCCNS(=O)(C4=CC=CC([C@@H]5CN(C)CC6=C5C=C(Cl)C=C6Cl)=C4)=O)=O)=O)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,145.04 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Markham A. Tenapanor: First Approval. Drugs. 2019 Nov;79(17):1897-1903. doi: 10.1007/s40265-019-01215-9. Review. PubMed PMID: 31677150.

2: Block GA, Rosenbaum DP, Yan A, Chertow GM. Efficacy and Safety of Tenapanor in Patients with Hyperphosphatemia Receiving Maintenance Hemodialysis: A Randomized Phase 3 Trial. J Am Soc Nephrol. 2019 Apr;30(4):641-652. doi: 10.1681/ASN.2018080832. Epub 2019 Mar 7. PubMed PMID: 30846557; PubMed Central PMCID: PMC6442342.

3: Kothari S, Vippagunta RR. Predicting the Physical Stability of Amorphous Tenapanor Hydrochloride Using Local Molecular Structure Analysis, Relaxation Time Constants, and Molecular Modeling. Mol Pharm. 2019 Mar 4;16(3):943-951. doi: 10.1021/acs.molpharmaceut.8b00853. Epub 2019 Feb 14. PubMed PMID: 30699296.

4: King AJ, Siegel M, He Y, Nie B, Wang J, Koo-McCoy S, Minassian NA, Jafri Q, Pan D, Kohler J, Kumaraswamy P, Kozuka K, Lewis JG, Dragoli D, Rosenbaum DP, O'Neill D, Plain A, Greasley PJ, Jönsson-Rylander AC, Karlsson D, Behrendt M, Strömstedt M, Ryden-Bergsten T, Knöpfel T, Pastor Arroyo EM, Hernando N, Marks J, Donowitz M, Wagner CA, Alexander RT, Caldwell JS. Inhibition of sodium/hydrogen exchanger 3 in the gastrointestinal tract by tenapanor reduces paracellular phosphate permeability. Sci Transl Med. 2018 Aug 29;10(456). pii: eaam6474. doi: 10.1126/scitranslmed.aam6474. PubMed PMID: 30158152; PubMed Central PMCID: PMC6454550.

5: Block GA, Rosenbaum DP, Yan A, Greasley PJ, Chertow GM, Wolf M. The effects of tenapanor on serum fibroblast growth factor 23 in patients receiving hemodialysis with hyperphosphatemia. Nephrol Dial Transplant. 2019 Feb 1;34(2):339-346. doi: 10.1093/ndt/gfy061. PubMed PMID: 29617976; PubMed Central PMCID: PMC6365767.

6: Nilsson Lill SO, Widdifield CM, Pettersen A, Svensk Ankarberg A, Lindkvist M, Aldred P, Gracin S, Shankland N, Shankland K, Schantz S, Emsley L. Elucidating an Amorphous Form Stabilization Mechanism for Tenapanor Hydrochloride: Crystal Structure Analysis Using X-ray Diffraction, NMR Crystallography, and Molecular Modeling. Mol Pharm. 2018 Apr 2;15(4):1476-1487. doi: 10.1021/acs.molpharmaceut.7b01047. Epub 2018 Mar 12. PubMed PMID: 29490140.

7: Rosenbaum DP, Yan A, Jacobs JW. Pharmacodynamics, Safety, and Tolerability of the NHE3 Inhibitor Tenapanor: Two Trials in Healthy Volunteers. Clin Drug Investig. 2018 Apr;38(4):341-351. doi: 10.1007/s40261-017-0614-0. PubMed PMID: 29363027; PubMed Central PMCID: PMC5856883.

8: Visconti L, Cernaro V, Calimeri S, Lacquaniti A, De Gregorio F, Ricciardi CA, Lacava V, Santoro D, Buemi M. The Myth of Water and Salt: From Aquaretics to Tenapanor. J Ren Nutr. 2018 Mar;28(2):73-82. doi: 10.1053/j.jrn.2017.06.005. Epub 2017 Nov 14. Review. PubMed PMID: 29146141.

9: Johansson S, Rosenbaum DP, Palm J, Stefansson B, Knutsson M, Lisbon EA, Hilgendorf C. Tenapanor administration and the activity of the H(+) -coupled transporter PepT1 in healthy volunteers. Br J Clin Pharmacol. 2017 Sep;83(9):2008-2014. doi: 10.1111/bcp.13313. Epub 2017 May 31. PubMed PMID: 28432691; PubMed Central PMCID: PMC5582369.

10: Johansson SA, Knutsson M, Leonsson-Zachrisson M, Rosenbaum DP. Effect of Food Intake on the Pharmacodynamics of Tenapanor: A Phase 1 Study. Clin Pharmacol Drug Dev. 2017 Sep;6(5):457-465. doi: 10.1002/cpdd.341. Epub 2017 Mar 24. PubMed PMID: 28339149; PubMed Central PMCID: PMC5599956.

11: Johansson S, Rosenbaum DP, Ahlqvist M, Rollison H, Knutsson M, Stefansson B, Elebring M. Effects of Tenapanor on Cytochrome P450-Mediated Drug-Drug Interactions. Clin Pharmacol Drug Dev. 2017 Sep;6(5):466-475. doi: 10.1002/cpdd.346. Epub 2017 Mar 16. PubMed PMID: 28301096; PubMed Central PMCID: PMC5599994.

12: Chey WD, Lembo AJ, Rosenbaum DP. Tenapanor Treatment of Patients With Constipation-Predominant Irritable Bowel Syndrome: A Phase 2, Randomized, Placebo-Controlled Efficacy and Safety Trial. Am J Gastroenterol. 2017 May;112(5):763-774. doi: 10.1038/ajg.2017.41. Epub 2017 Feb 28. PubMed PMID: 28244495; PubMed Central PMCID: PMC5418559.

13: Carney EF. Dialysis: Efficacy of tenapanor in hyperphosphataemia. Nat Rev Nephrol. 2017 Apr;13(4):194. doi: 10.1038/nrneph.2017.27. Epub 2017 Feb 27. PubMed PMID: 28239171.

14: Block GA, Rosenbaum DP, Leonsson-Zachrisson M, Åstrand M, Johansson S, Knutsson M, Langkilde AM, Chertow GM. Effect of Tenapanor on Serum Phosphate in Patients Receiving Hemodialysis. J Am Soc Nephrol. 2017 Jun;28(6):1933-1942. doi: 10.1681/ASN.2016080855. Epub 2017 Feb 3. PubMed PMID: 28159782; PubMed Central PMCID: PMC5461797.

15: Johansson S, Leonsson-Zachrisson M, Knutsson M, Spencer AG, Labonté ED, Deshpande D, Kohler J, Kozuka K, Charmot D, Rosenbaum DP. Preclinical and Healthy Volunteer Studies of Potential Drug-Drug Interactions Between Tenapanor and Phosphate Binders. Clin Pharmacol Drug Dev. 2017 Sep;6(5):448-456. doi: 10.1002/cpdd.307. Epub 2016 Oct 26. PubMed PMID: 27654985; PubMed Central PMCID: PMC5599948.

16: Johansson S, Rosenbaum DP, Knutsson M, Leonsson-Zachrisson M. A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers. Clin Exp Nephrol. 2017 Jun;21(3):407-416. doi: 10.1007/s10157-016-1302-8. Epub 2016 Jul 1. PubMed PMID: 27368672; PubMed Central PMCID: PMC5486465.

17: Block GA, Rosenbaum DP, Leonsson-Zachrisson M, Stefansson BV, Rydén-Bergsten T, Greasley PJ, Johansson SA, Knutsson M, Carlsson BC. Effect of Tenapanor on Interdialytic Weight Gain in Patients on Hemodialysis. Clin J Am Soc Nephrol. 2016 Sep 7;11(9):1597-605. doi: 10.2215/CJN.09050815. Epub 2016 Jun 23. PubMed PMID: 27340281; PubMed Central PMCID: PMC5012484.

18: Zielińska M, Wasilewski A, Fichna J. Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome. Expert Opin Investig Drugs. 2015;24(8):1093-9. doi: 10.1517/13543784.2015.1054480. Epub 2015 Jun 12. Review. PubMed PMID: 26065434.