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MedKoo Cat#: 206127 | Name: Tradipitant
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Description:

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

Tradipitant, also known as VLY-686 and LY686017, is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models. LY686017 may be a possible therapy for alcoholism. LY686017 can be also served as a suitable chemical platform for future imaging ligand development.

Chemical Structure

Tradipitant
Tradipitant
CAS#622370-35-8

Theoretical Analysis

MedKoo Cat#: 206127

Name: Tradipitant

CAS#: 622370-35-8

Chemical Formula: C28H16ClF6N5O

Exact Mass: 587.0948

Molecular Weight: 587.90

Elemental Analysis: C, 57.20; H, 2.74; Cl, 6.03; F, 19.39; N, 11.91; O, 2.72

Price and Availability

Size Price Availability Quantity
25mg USD 550.00 2 Weeks
100mg USD 1,650.00 2 Weeks
1g USD 4,650.00 2 Weeks
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Related CAS #
No Data
Synonym
Tradipitant; LY686017; LY 686017; LY686017; VLY 686; VLY686; VLY686.
IUPAC/Chemical Name
(2-(1-(3,5-bis(trifluoromethyl)benzyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)pyridin-3-yl)(2-chlorophenyl)methanone
InChi Key
CAVRKWRKTNINFF-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H16ClF6N5O/c29-22-6-2-1-4-20(22)26(41)21-5-3-9-37-23(21)24-25(17-7-10-36-11-8-17)40(39-38-24)15-16-12-18(27(30,31)32)14-19(13-16)28(33,34)35/h1-14H,15H2
SMILES Code
O=C(C1=CC=CN=C1C2=C(C3=CC=NC=C3)N(CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)N=N2)C5=CC=CC=C5Cl
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, not in water
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
        

Preparing Stock Solutions

The following data is based on the product molecular weight 587.90 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
1: Freisthler B, Chahine RA, Villani J, Chandler R, Feaster DJ, Slavova S, Defiore-Hyrmer J, Walley AY, Kosakowski S, Aldridge A, Barbosa C, Bhatta S, Brancato C, Bridden C, Christopher M, Clarke T, David J, D'Costa L, Ewing I, Fernandez S, Gibson E, Gilbert L, Hall ME, Hargrove S, Hunt T, Kinnard EN, Larochelle L, Macoubray A, Nigam S, Nunes EV, Oser CB, Pagnano S, Rock P, Salsberry P, Shadwick A, Stopka TJ, Tan S, Taylor JL, Westgate PM, Wu E, Zarkin GA, Walsh SL, El-Bassel N, Winhusen TJ, Samet JH, Oga EA. Communities That HEAL Intervention and Mortality Including Polysubstance Overdose Deaths: A Randomized Clinical Trial. JAMA Netw Open. 2024 Oct 1;7(10):e2440006. doi: 10.1001/jamanetworkopen.2024.40006. PMID: 39432308; PMCID: PMC11581668. 2: D'Onofrio G, Herring AA, Perrone J, Hawk K, Samuels EA, Cowan E, Anderson E, McCormack R, Huntley K, Owens P, Martel S, Schactman M, Lofwall MR, Walsh SL, Dziura J, Fiellin DA. Extended-Release 7-Day Injectable Buprenorphine for Patients With Minimal to Mild Opioid Withdrawal. JAMA Netw Open. 2024 Jul 1;7(7):e2420702. doi: 10.1001/jamanetworkopen.2024.20702. PMID: 38976265; PMCID: PMC11231806. 3: Nunes EV, Comer SD, Lofwall MR, Walsh SL, Peterson S, Tiberg F, Hjelmstrom P, Budilovsky-Kelley NR. Extended-Release Injection vs Sublingual Buprenorphine for Opioid Use Disorder With Fentanyl Use: A Post Hoc Analysis of a Randomized Clinical Trial. JAMA Netw Open. 2024 Jun 3;7(6):e2417377. doi: 10.1001/jamanetworkopen.2024.17377. PMID: 38916892; PMCID: PMC11200143. 4: Stopka TJ, Babineau DC, Gibson EB, Knott CE, Cheng DM, Villani J, Wai JM, Blevins D, David JL, Goddard-Eckrich DA, Lofwall MR, Massatti R, DeFiore-Hyrmer J, Lyons MS, Fanucchi LC, Harris DR, Talbert J, Hammerslag L, Oller D, Balise RR, Feaster DJ, Soares W, Zarkin GA, Glasgow L, Oga E, McCarthy J, D'Costa L, Chahine R, Gomori S, Dalvi N, Shrestha S, Garner C, Shadwick A, Salsberry P, Konstan MW, Freisthler B, Winhusen J, El-Bassel N, Samet JH, Walsh SL. Impact of the Communities That HEAL Intervention on Buprenorphine-Waivered Practitioners and Buprenorphine Prescribing: A Prespecified Secondary Analysis of the HCS Randomized Clinical Trial. JAMA Netw Open. 2024 Feb 5;7(2):e240132. doi: 10.1001/jamanetworkopen.2024.0132. Erratum in: JAMA Netw Open. 2024 Aug 1;7(8):e2433598. doi: 10.1001/jamanetworkopen.2024.33598. PMID: 38386322; PMCID: PMC10884876. 5: Carlin JL, Polymeropoulos C, Camilleri M, Lembo A, Fisher M, Kupersmith C, Madonick D, Moszczynski P, Smieszek S, Xiao C, Birznieks G, Polymeropoulos MH. The Efficacy of Tradipitant in Patients With Diabetic and Idiopathic Gastroparesis in a Phase 3 Randomized Placebo-Controlled Clinical Trial. Clin Gastroenterol Hepatol. 2024 Dec;22(12):2506-2516. doi: 10.1016/j.cgh.2024.01.005. Epub 2024 Jan 17. PMID: 38237696. 6: Zahid SA, Tated R, Mathew M, Rajkumar D, Karnik SB, Pramod Roy A, Jacob FP, Baskara Salian R, Razzaq W, Shivakumar D, Khawaja UA. Diabetic Gastroparesis and its Emerging Therapeutic Options: A Narrative Review of the Literature. Cureus. 2023 Sep 7;15(9):e44870. doi: 10.7759/cureus.44870. PMID: 37814758; PMCID: PMC10560130. 7: Czeisler MÉ, Pruski JM, Wang P, Wang J, Xiao C, Polymeropoulos MH, Polymeropoulos VM. Validation of the motion sickness severity scale: Secondary analysis of a randomized, double-blind, placebo-controlled study of a treatment for motion sickness. PLoS One. 2023 Jan 5;18(1):e0280058. doi: 10.1371/journal.pone.0280058. PMID: 36602998; PMCID: PMC9815635. 8: Ehrenpreis ED, Kruchko DH. Editorial: tradipitant has promise for treating gastroparesis but leaves gastric function alone. Aliment Pharmacol Ther. 2022 Aug;56(3):540-541. doi: 10.1111/apt.17090. PMID: 35804474. 9: Camilleri M, Zheng T. Editorial: tradipitant has promise for treating gastroparesis but leaves gastric function alone-authors' reply. Aliment Pharmacol Ther. 2022 Aug;56(3):542-543. doi: 10.1111/apt.17098. PMID: 35804471. 10: Khanna L, Zheng T, Atieh J, Torres M, Busciglio I, Carlin JL, Xiao M, Harmsen WS, Camilleri M. Clinical trial: a single-centre, randomised, controlled trial of tradipitant on satiation, gastric functions, and serum drug levels in healthy volunteers. Aliment Pharmacol Ther. 2022 Jul;56(2):224-230. doi: 10.1111/apt.17065. Epub 2022 May 29. PMID: 35644931. 11: Smieszek SP, Przychodzen BP, Polymeropoulos VM, Polymeropoulos CM, Polymeropoulos MH. Assessing the potential correlation of polymorphisms in the IL6R with relative IL6 elevation in severely ill COVID-19 patients'. Cytokine. 2021 Dec;148:155662. doi: 10.1016/j.cyto.2021.155662. Epub 2021 Jul 29. Erratum in: Cytokine. 2022 Jan;149:155752. doi: 10.1016/j.cyto.2021.155752. PMID: 34353696; PMCID: PMC8318728. 12: Coe MA, Lofwall MR, Vessels V, Nuzzo PA, Walsh SL. Evaluation of tradipitant, a selective NK1 antagonist, on response to oxycodone in humans. Psychopharmacology (Berl). 2021 Jul;238(7):1857-1866. doi: 10.1007/s00213-021-05814-x. Epub 2021 May 14. PMID: 33988725; PMCID: PMC8120018. 13: Wang XJ, Burton DD, Breen-Lyles M, Camilleri M. Gastric accommodation influences proximal gastric and total gastric emptying in concurrent measurements conducted in healthy volunteers. Am J Physiol Gastrointest Liver Physiol. 2021 May 1;320(5):G759-G767. doi: 10.1152/ajpgi.00008.2021. Epub 2021 Mar 10. PMID: 33719546; PMCID: PMC8202200. 14: Camilleri M. Relationship of motor mechanisms to gastroparesis symptoms: toward individualized treatment. Am J Physiol Gastrointest Liver Physiol. 2021 Apr 1;320(4):G558-G563. doi: 10.1152/ajpgi.00006.2021. Epub 2021 Feb 10. PMID: 33566731; PMCID: PMC8238170. 15: Welsh SE, Xiao C, Kaden AR, Brzezynski JL, Mohrman MA, Wang J, Smieszek SP, Przychodzen B, Ständer S, Polymeropoulos C, Birznieks G, Polymeropoulos MH. Neurokinin-1 receptor antagonist tradipitant has mixed effects on itch in atopic dermatitis: results from EPIONE, a randomized clinical trial. J Eur Acad Dermatol Venereol. 2021 May;35(5):e338-e340. doi: 10.1111/jdv.17090. Epub 2021 Jan 7. PMID: 33330999; PMCID: PMC8248080. 16: Polymeropoulos VM, Czeisler MÉ, Gibson MM, Anderson AA, Miglo J, Wang J, Xiao C, Polymeropoulos CM, Birznieks G, Polymeropoulos MH. Tradipitant in the Treatment of Motion Sickness: A Randomized, Double-Blind, Placebo-Controlled Study. Front Neurol. 2020 Sep 29;11:563373. doi: 10.3389/fneur.2020.563373. PMID: 33117260; PMCID: PMC7550735. 17: Carlin JL, Lieberman VR, Dahal A, Keefe MS, Xiao C, Birznieks G, Abell TL, Lembo A, Parkman HP, Polymeropoulos MH. Efficacy and Safety of Tradipitant in Patients With Diabetic and Idiopathic Gastroparesis in a Randomized, Placebo- Controlled Trial. Gastroenterology. 2021 Jan;160(1):76-87.e4. doi: 10.1053/j.gastro.2020.07.029. Epub 2020 Jul 18. PMID: 32693185. 18: Chu CY. Treatments for Childhood Atopic Dermatitis: an Update on Emerging Therapies. Clin Rev Allergy Immunol. 2021 Oct;61(2):114-127. doi: 10.1007/s12016-020-08799-1. PMID: 32607924. 19: Pojawa-Gołąb M, Jaworecka K, Reich A. NK-1 Receptor Antagonists and Pruritus: Review of Current Literature. Dermatol Ther (Heidelb). 2019 Sep;9(3):391-405. doi: 10.1007/s13555-019-0305-2. Epub 2019 Jun 12. PMID: 31190215; PMCID: PMC6704190.

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