Tenapanor free base | AZD-1722 | CAS#1234423-95-0 | 1234365-97-9 | Na+/H+ exchanger 3 (NHE3) inhibitor

MedKoo Cat#: 329611 | Name: Tenapanor free base

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

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: 1142.3097

Molecular Weight: 1145.04

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
50mg	USD 550.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,650.00	2 Weeks
500mg	USD 3,250.00	2 Weeks
1g	USD 4,850.00	2 Weeks
2g	USD 7,450.00	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

Instruction

View handling instruction

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.

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

1: Yu S, Sun J, Guo X. Efficacy and safety of tenapanor in end-stage renal disease patients with hyperphosphatemia: a systematic review and meta-analysis. Ren Fail. 2024 Dec;46(2):2410389. doi: 10.1080/0886022X.2024.2410389. Epub 2024 Oct 1. PMID: 39351794; PMCID: PMC11445914. 2: Efficacy of Tenapanor in Patients With IBS-C: A Post Hoc Analysis of Patients With and Without Prior Use of Other IBS-C Prescription Medications From the Phase 3 T3MPO 1 and T3MPO-2 Studies. Gastroenterol Hepatol (N Y). 2024 Jul;20(7 Suppl 4):2-3. PMID: 39193437; PMCID: PMC11345968. 3: Comparing the Efficacy of Tenapanor in IBS-C in Hispanic Versus Non-Hispanic Patients: A Post Hoc Analysis of Patients in the Phase 3 T3MPO-1 and T3MPO-2 Studies. Gastroenterol Hepatol (N Y). 2024 Jul;20(7 Suppl 4):4-5. PMID: 39193434; PMCID: PMC11345969. 4: Sendzischew Shane MA, Ruddy J, Cline M, Rosenbaum DP, Edelstein S, Moshiree B. Review of the Patient Burden and Therapeutic Landscape of Irritable Bowel Syndrome with Constipation in the United States. Clin Exp Gastroenterol. 2024 Aug 2;17:227-253. doi: 10.2147/CEG.S464375. Erratum in: Clin Exp Gastroenterol. 2024 Nov 20;17:347-348. doi: 10.2147/CEG.S506887. PMID: 39114809; PMCID: PMC11303673. 5: Soeda K, Komaba H. Navigating How to Initiate Tenapanor Therapy in the Real World. Kidney360. 2024 Jul 1;5(7):938-940. doi: 10.34067/KID.0000000000000488. PMID: 39052472; PMCID: PMC11296554. 6: Silva A, Edelstein S, Yang Y, Rosenbaum D, Battelli L, Chertow GM. Tenapanor improves long-term control of high phosphate concentrations in the blood in patients receiving maintenance dialysis: a plain language summary of the NORMALIZE study. Curr Med Res Opin. 2024 Aug;40(8):1345-1356. doi: 10.1080/03007995.2024.2364824. Epub 2024 Jul 23. PMID: 39041778. 7: Sprague SM, Edelstein S, Spiegel DM, Rosenbaum DP, Thomas C, Weiner DE. Effectiveness of tenapanor for treating hyperphosphatemia in patients receiving dialysis: a plain language summary of the OPTIMIZE study. Curr Med Res Opin. 2024 Aug;40(8):1335-1343. doi: 10.1080/03007995.2024.2364815. Epub 2024 Jul 23. PMID: 39041739. 8: Hill Gallant KM, Sprague SM, Rosenbaum DP, Spiegel DM, Kozuka K, Edelstein S, Chertow GM. Tenapanor: A Phosphate Absorption Inhibitor for the Management of Hyperphosphatemia in Patients With Kidney Failure. J Ren Nutr. 2024 Jul 9:S1051-2276(24)00156-0. doi: 10.1053/j.jrn.2024.07.003. Epub ahead of print. PMID: 38992521. 9: Lacy BE, Rosenbaum D, Edelstein S, Kozuka K, Williams LA, Kunkel DC. Intestinal Permeability, Irritable Bowel Syndrome with Constipation, and the Role of Sodium-Hydrogen Exchanger Isoform 3 (NHE3). Clin Exp Gastroenterol. 2024 Jun 6;17:173-183. doi: 10.2147/CEG.S455101. PMID: 38860153; PMCID: PMC11164200. 10: Cernaro V, Longhitano E, Casuscelli C, Peritore L, Santoro D. Hyperphosphatemia in Chronic Kidney Disease: The Search for New Treatment Paradigms and the Role of Tenapanor. Int J Nephrol Renovasc Dis. 2024 May 28;17:151-161. doi: 10.2147/IJNRD.S385826. PMID: 38831770; PMCID: PMC11144652. 11: Singh P, Sayuk GS, Rosenbaum DP, Edelstein S, Kozuka K, Chang L. An Overview of the Effects of Tenapanor on Visceral Hypersensitivity in the Treatment of Irritable Bowel Syndrome with Constipation. Clin Exp Gastroenterol. 2024 Apr 10;17:87-96. doi: 10.2147/CEG.S454526. PMID: 38617992; PMCID: PMC11016248. 12: Lembo AJ, Edelstein S, Rosenbaum DP, Rooker C, Roberts JD, Chey WD. Long- term safety of tenapanor in people with irritable bowel syndrome with constipation from the T3MPO-3 study: plain language summary of publication. Therap Adv Gastroenterol. 2024 Apr 9;17:17562848241237196. doi: 10.1177/17562848241237196. PMID: 38601815; PMCID: PMC11005483. 13: Yuan G, Chen Y, Li L, Wang X, Wei G, Zeng J, Hui AM, Jiang Y, Zhao H, Diao L, Zhou Y, Xiao Y, Chen M. Pharmacokinetics, Safety, and Tolerability of Tenapanor in Healthy Chinese and Caucasian Volunteers: A Randomized, Open-Label, Single-Center, Placebo-Controlled Phase 1 Study. Int J Clin Pract. 2024 Mar 6;2024:1386980. doi: 10.1155/2024/1386980. PMID: 38481823; PMCID: PMC10937073. 14: Dominguez Rieg JA, Rieg T. New functions and roles of the Na+-H+-exchanger NHE3. Pflugers Arch. 2024 Apr;476(4):505-516. doi: 10.1007/s00424-024-02938-9. Epub 2024 Mar 7. PMID: 38448727. 15: Tenapanor (Xphozah) for hyperphosphatemia in chronic kidney disease. Med Lett Drugs Ther. 2024 Mar 4;66(1697):38-39. doi: 10.58347/tml.2024.1697b. PMID: 38412277. 16: Sprague SM, Weiner DE, Tietjen DP, Pergola PE, Fishbane S, Block GA, Silva AL, Fadem SZ, Lynn RI, Fadda G, Pagliaro L, Zhao S, Edelstein S, Spiegel DM, Rosenbaum DP. Tenapanor as Therapy for Hyperphosphatemia in Maintenance Dialysis Patients: Results from the OPTIMIZE Study. Kidney360. 2024 May 1;5(5):732-742. doi: 10.34067/KID.0000000000000387. Epub 2024 Feb 7. PMID: 38323855; PMCID: PMC11146652. 17: Lembo AJ, Chey WD, Harris LA, Frazier R, Brenner DM, Chang L, Lacy BE, Edelstein S, Yang Y, Zhao S, Rosenbaum DP. Abdominal Symptom Improvement During Clinical Trials of Tenapanor in Patients With Irritable Bowel Syndrome With Constipation: A Post Hoc Analysis. Am J Gastroenterol. 2024 May 1;119(5):937-945. doi: 10.14309/ajg.0000000000002685. Epub 2024 Jan 31. PMID: 38294158; PMCID: PMC11062617. 18: King AJ, Chang L, Li Q, Liu L, Zhu Y, Pasricha PJ, Wang J, Siegel M, Caldwell JS, Edelstein S, Rosenbaum DP, Kozuka K. NHE3 inhibitor tenapanor maintains intestinal barrier function, decreases visceral hypersensitivity, and attenuates TRPV1 signaling in colonic sensory neurons. Am J Physiol Gastrointest Liver Physiol. 2024 May 1;326(5):G543-G554. doi: 10.1152/ajpgi.00233.2023. Epub 2024 Jan 22. PMID: 38252683; PMCID: PMC11376972. 19: Gan L, Xing L, Xu Y, Zhou L, Jiang H, Sun X, Guan T, Luo P, Wang J, Sun F, Guo Z, Guo M, Gao J, Wei G, Zhong W, Zhou Y, Zuo L. Tenapanor in Chinese ESRD patients with hyperphosphatemia on haemodialysis: a randomised, phase 3 trial. Clin Kidney J. 2023 Oct 11;17(1):sfad216. doi: 10.1093/ckj/sfad216. PMID: 38186905; PMCID: PMC10768776. 20: Stamatopoulos K, Mistry N, Fotaki N, Turner DB, Swift B. Physiologically Based Biopharmaceutics Model (PBBM) of Minimally Absorbed Locally Acting Drugs in the Gastrointestinal Tract-Case Study: Tenapanor. Pharmaceutics. 2023 Dec 4;15(12):2726. doi: 10.3390/pharmaceutics15122726. PMID: 38140067; PMCID: PMC10747343.