Eliapixant | CAS# 1948229-21-7 | P2X3 receptor antagonist

MedKoo Cat#: 574268 | Name: Eliapixant

Description:

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

Eliapixant, also known as BAY 1817080, is a P2X3 receptor antagonist. Eliapixant is both highly potent and selective for P2X3 over other P2X subtypes in vitro, including P2X2/3. Eliapixant reduces inflammatory pain in relevant animal models. P2X3 antagonism reduces neurogenic inflammation, a phenomenon hypothesised to contribute to several diseases, including endometriosis. P2X3 antagonism could alleviate pain, including non-menstrual pelvic pain, and modify the underlying disease pathophysiology in women with endometriosis. Eliapixant is currently under clinical development for the treatment of disorders associated with hypersensitive nerve fibers.

Chemical Structure

Eliapixant

CAS#1948229-21-7

Theoretical Analysis

MedKoo Cat#: 574268

Name: Eliapixant

CAS#: 1948229-21-7

Chemical Formula: C22H21F3N4O3S

Exact Mass: 478.1286

Molecular Weight: 478.49

Elemental Analysis: C, 55.22; H, 4.42; F, 11.91; N, 11.71; O, 10.03; S, 6.70

Price and Availability

Size	Price	Availability
50mg	USD 950.00	2 Weeks
100mg	USD 1,650.00	2 Weeks
200mg	USD 2,650.00	2 Weeks
500mg	USD 4,650.00	2 Weeks
1g	USD 6,950.00	2 Weeks
2g	USD 11,650.00	2 Weeks

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Related CAS #

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Synonym

Eliapixant; BAY 1817080; BAY-1817080; BAY1817080;

IUPAC/Chemical Name

3-(5-methyl-1,3-thiazol-2-yl)-5-{[(3R)-oxolan-3-yl]oxy}-N-{(1R)-1-[2-(trifluoromethyl)pyrimidin-5- yl]ethyl}benzamide

InChi Key

GTQPEQGDLVSFJO-CXAGYDPISA-N

InChi Code

InChI=1S/C22H21F3N4O3S/c1-12-8-26-20(33-12)15-5-14(6-18(7-15)32-17-3-4-31-11-17)19(30)29-13(2)16-9-27-21(28-10-16)22(23,24)25/h5-10,13,17H,3-4,11H2,1-2H3,(H,29,30)/t13-,17-/m1/s1

SMILES Code

O=C(N[C@@H](C1=CN=C(C(F)(F)F)N=C1)C)C2=CC(O[C@H]3COCC3)=CC(C4=NC=C(C)S4)=C2

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

>3 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 478.49 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: Morice A, Smith JA, McGarvey L, Birring SS, Parker SM, Turner A, Hummel T, Gashaw I, Fels L, Klein S, Francke K, Friedrich C. Eliapixant (BAY 1817080), a P2X3 receptor antagonist, in refractory chronic cough: a randomised, placebo- controlled, crossover phase 2a study. Eur Respir J. 2021 Nov 18;58(5):2004240. doi: 10.1183/13993003.04240-2020. PMID: 33986030; PMCID: PMC8607926. 2: Davenport AJ, Neagoe I, Bräuer N, Koch M, Rotgeri A, Nagel J, Laux-Biehlmann A, Machet F, Coelho AM, Boyce S, Carty N, Gemkow MJ, Hess SD, Zollner TM, Fischer OM. Eliapixant is a selective P2X3 receptor antagonist for the treatment of disorders associated with hypersensitive nerve fibers. Sci Rep. 2021 Oct 6;11(1):19877. doi: 10.1038/s41598-021-99177-0. PMID: 34615939; PMCID: PMC8494816. 3: Klein S, Gashaw I, Baumann S, Chang X, Hummel T, Thuß U, Friedrich C. First- in-human study of eliapixant (BAY 1817080), a highly selective P2X3 receptor antagonist: Tolerability, safety and pharmacokinetics. Br J Clin Pharmacol. 2022 Oct;88(10):4552-4564. doi: 10.1111/bcp.15358. Epub 2022 May 22. PMID: 35437837; PMCID: PMC9546310. 4: Dicpinigaitis PV, Morice AH, Smith JA, Sher MR, Vaezi M, Guilleminault L, Niimi A, Gude K, Krahn U, Saarinen R, Pires PV, Wosnitza M, McGarvey L; PAGANINI Investigators. Efficacy and Safety of Eliapixant in Refractory Chronic Cough: The Randomized, Placebo-Controlled Phase 2b PAGANINI Study. Lung. 2023 Jun;201(3):255-266. doi: 10.1007/s00408-023-00621-x. Epub 2023 Jun 1. PMID: 37261531; PMCID: PMC10234230. 5: Ewerton F, Cruz F, Kapp M, Klein S, Roehm P, Chapple C. Efficacy and Safety of Eliapixant in Overactive Bladder: The 12-Week, Randomised, Placebo-controlled Phase 2a OVADER Study. Eur Urol Focus. 2023 Aug 8:S2405-4569(23)00182-7. doi: 10.1016/j.euf.2023.07.008. Epub ahead of print. PMID: 37563004. 6: Fletcher MC. Selectivity of the P2X3 receptor antagonist Eliapixant, and its potential use in the treatment of endometriosis. Purinergic Signal. 2022 Mar;18(1):1-3. doi: 10.1007/s11302-021-09831-5. Epub 2022 Jan 3. PMID: 34978027; PMCID: PMC8850518. 7: Friedrich C, Francke K, Gashaw I, Scheerans C, Klein S, Fels L, Smith JA, Hummel T, Morice A. Safety, Pharmacodynamics, and Pharmacokinetics of P2X3 Receptor Antagonist Eliapixant (BAY 1817080) in Healthy Subjects: Double-Blind Randomized Study. Clin Pharmacokinet. 2022 Aug;61(8):1143-1156. doi: 10.1007/s40262-022-01126-1. Epub 2022 May 28. PMID: 35624408; PMCID: PMC9349145. 8: Francke K, Chattopadhyay N, Klein S, Rottmann A, Krickau D, van de Wetering J, Friedrich C. Preclinical and Clinical Pharmacokinetics and Bioavailability in Healthy Volunteers of a Novel Formulation of the Selective P2X3 Receptor Antagonist Eliapixant. Eur J Drug Metab Pharmacokinet. 2023 Jan;48(1):75-87. doi: 10.1007/s13318-022-00805-5. Epub 2022 Dec 5. PMID: 36469250. 9: Sluyter R, Sophocleous RA, Stokes L. P2X receptors: Insights from the study of the domestic dog. Neuropharmacology. 2023 Feb 15;224:109358. doi: 10.1016/j.neuropharm.2022.109358. Epub 2022 Dec 1. PMID: 36464207. 10: Yi B, Wang S, Li W, Xu X, Yu L. Potential applications of P2X3 receptor antagonists in the treatment of refractory cough. Respir Med. 2023 Oct;217:107336. doi: 10.1016/j.rmed.2023.107336. Epub 2023 Jun 25. PMID: 37364722. 11: Zheng Z, Huang J, Xiang Z, Wu T, Lan X, Xie S, Lin Z, Tang K, Morice A, Li S, Song WJ, Chen R. Efficacy and safety of pharmacotherapy for refractory or unexplained chronic cough: a systematic review and network meta-analysis. EClinicalMedicine. 2023 Jul 20;62:102100. doi: 10.1016/j.eclinm.2023.102100. PMID: 37538538; PMCID: PMC10393600. 12: Ramadan A, El-Samahy M, Elrosasy A, Al-Tawil M, Abdelaziz A, Soliman MA, Abouzid M. Safety and efficacy of P2X3 receptor antagonist for the treatment of refractory or unexplained chronic cough: A systematic review and meta-analysis of 11 randomized controlled trials. Pulm Pharmacol Ther. 2023 Sep 9;83:102252. doi: 10.1016/j.pupt.2023.102252. Epub ahead of print. PMID: 37678663.