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MedKoo Cat#: 535190 | Name: Danavorexton
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Description:

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

Danavorexton, also known as TAK 925, is an orexin receptor agonist. TAK-925 activated human recombinant OX2R with 50% effective concentration value of 5.5 nM, and showed >5,000-fold selectivity over OX1R in calcium mobilization assays. TAK-925 induced OX2R-downstream signals similar to those displayed by orexin peptides in Chinese hamster ovary cells stably expressing human OX2R. In an electrophysiological study, TAK-925 activated physiological OX2R on histaminergic neurons in the mouse tuberomammillary nucleus (TMN). Subcutaneous (SC) administration of TAK-925 also modulated neuronal activity in various brain regions, including TMN, as measured by an immunohistochemical analysis using an anti-c-fos antibody. TAK-925 (SC) increased wakefulness in wild-type mice, but not in OX2R KO mice, during their sleep phase, demonstrating that a highly selective OX2R agonist can increase wakefulness in mice via OX2R activation. TAK-925 may have therapeutic potential to reduce hypersomnia in multiple disorders including NT1.

Chemical Structure

Danavorexton
Danavorexton
CAS#2114324-48-8

Theoretical Analysis

MedKoo Cat#: 535190

Name: Danavorexton

CAS#: 2114324-48-8

Chemical Formula: C21H32N2O5S

Exact Mass: 424.2032

Molecular Weight: 424.56

Elemental Analysis: C, 59.41; H, 7.60; N, 6.60; O, 18.84; S, 7.55

Price and Availability

Size Price Availability Quantity
5mg USD 1,250.00 2 Weeks
10mg USD 2,050.00 2 Weeks
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Related CAS #
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Synonym
Danavorexton; TAK 925; TAK-925; TAK925;
IUPAC/Chemical Name
methyl (2R,3S)-3-(methanesulfonamido)-2-{[(cis-4-phenylcyclohexyl)oxy]methyl}piperidine-1-carboxylate
InChi Key
UXZAJSZFFARTEI-YRPNKDGESA-N
InChi Code
InChI=1S/C21H32N2O5S/c1-27-21(24)23-14-6-9-19(22-29(2,25)26)20(23)15-28-18-12-10-17(11-13-18)16-7-4-3-5-8-16/h3-5,7-8,17-20,22H,6,9-15H2,1-2H3/t17-,18+,19-,20-/m0/s1
SMILES Code
O=C(N1[C@@H](CO[C@H]2CC[C@@H](C3=CC=CC=C3)CC2)[C@@H](NS(=O)(C)=O)CCC1)OC
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

Preparing Stock Solutions

The following data is based on the product molecular weight 424.56 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: Yin J, Kang Y, McGrath AP, Chapman K, Sjodt M, Kimura E, Okabe A, Koike T, Miyanohana Y, Shimizu Y, Rallabandi R, Lian P, Bai X, Flinspach M, De Brabander JK, Rosenbaum DM. Molecular mechanism of the wake-promoting agent TAK-925. Nat Commun. 2022 May 25;13(1):2902. doi: 10.1038/s41467-022-30601-3. PMID: 35614071; PMCID: PMC9133036. 2: Yukitake H, Fujimoto T, Ishikawa T, Suzuki A, Shimizu Y, Rikimaru K, Ito M, Suzuki M, Kimura H. TAK-925, an orexin 2 receptor-selective agonist, shows robust wake-promoting effects in mice. Pharmacol Biochem Behav. 2019 Dec;187:172794. doi: 10.1016/j.pbb.2019.172794. Epub 2019 Oct 22. PMID: 31654653. 3: Fujimoto T, Rikimaru K, Fukuda K, Sugimoto H, Masuda K, Ohyabu N, Banno Y, Tokunaga N, Kawamoto T, Tomata Y, Kumagai Y, Iida M, Nagano Y, Yoneyama-Hirozane M, Shimizu Y, Sasa K, Ishikawa T, Yukitake H, Ito M, Aoyama K, Matsumoto T. Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist. ACS Med Chem Lett. 2022 Feb 4;13(3):457-462. doi: 10.1021/acsmedchemlett.1c00626. PMID: 35295087; PMCID: PMC8919389. 4: Evans R, Kimura H, Nakashima M, Ishikawa T, Yukitake H, Suzuki M, Hazel J, Faessel H, Wu J, Hang Y, Alexander R, Rosen L, Hartman DS, Ratti E. Orexin 2 receptor-selective agonist danavorexton (TAK-925) promotes wakefulness in non- human primates and healthy individuals. J Sleep Res. 2023 Oct;32(5):e13878. doi: 10.1111/jsr.13878. Epub 2023 Mar 19. PMID: 36934366. 5: Sun Y, Ranjan A, Tisdale R, Ma SC, Park S, Haire M, Heu J, Morairty SR, Wang X, Rosenbaum DM, Williams NS, De Brabander JK, Kilduff TS. Evaluation of the efficacy of the hypocretin/orexin receptor agonists TAK-925 and ARN-776 in narcoleptic orexin/tTA; TetO-DTA mice. J Sleep Res. 2023 Aug;32(4):e13839. doi: 10.1111/jsr.13839. Epub 2023 Feb 20. PMID: 36808670; PMCID: PMC10356740. 6: Ishikawa T, Hara H, Kawano A, Kimura H. Danavorexton, a selective orexin 2 receptor agonist, provides a symptomatic improvement in a narcolepsy mouse model. Pharmacol Biochem Behav. 2022 Oct;220:173464. doi: 10.1016/j.pbb.2022.173464. Epub 2022 Sep 13. PMID: 36108771. 7: Kaku K, Enya K, Nakaya R, Ohira T, Matsuno R. Long-term safety and efficacy of fasiglifam (TAK-875), a G-protein-coupled receptor 40 agonist, as monotherapy and combination therapy in Japanese patients with type 2 diabetes: a 52-week open-label phase III study. Diabetes Obes Metab. 2016 Sep;18(9):925-9. doi: 10.1111/dom.12693. Epub 2016 Jun 29. PMID: 27178047. 8: Jabłonowska E, Szetela B, Bielecki M, Horban A, Bociąga-Jasik M, Mularska E, Hlebowicz M, Olczak A, Parczewski M, Grzeszczuk A, Bielec D, Cybula A, Kocbach- Przudzik A, Ankiersztejn-Bartczak M, Kowalska JD. Acquired immune deficiency syndrome (AIDS) and late presentation in Poland - data from Test and Keep in Care (TAK) Polska project. HIV Med. 2021 May;22(5):387-396. doi: 10.1111/hiv.13041. Epub 2021 Jan 6. PMID: 33410278. 9: Lin TZ, Jayasvasti I, Tiraphat S, Pengpid S, Jayasvasti M, Borriharn P. The Predictors Influencing the Rational Use of Antibiotics Among Public Sector: A Community-Based Survey in Thailand. Drug Healthc Patient Saf. 2022 Mar 25;14:27-36. doi: 10.2147/DHPS.S339808. PMID: 35369038; PMCID: PMC8965102. 10: Mossberg M, Segelmark M, Kahn R, Englund M, Mohammad AJ. Epidemiology of primary systemic vasculitis in children: a population-based study from southern Sweden. Scand J Rheumatol. 2018 Jul;47(4):295-302. doi: 10.1080/03009742.2017.1412497. Epub 2018 Feb 7. Erratum in: Scand J Rheumatol. 2018 Jul;47(4):344. PMID: 29409373. 11: Okano S, Ikeura Y, Inatomi N. Effects of tachykinin NK1 receptor antagonists on the viscerosensory response caused by colorectal distention in rabbits. J Pharmacol Exp Ther. 2002 Mar;300(3):925-31. doi: 10.1124/jpet.300.3.925. PMID: 11861799. 12: Tak WY, Ryoo BY, Lim HY, Kim DY, Okusaka T, Ikeda M, Hidaka H, Yeon JE, Mizukoshi E, Morimoto M, Lee MA, Yasui K, Kawaguchi Y, Heo J, Morita S, Kim TY, Furuse J, Katayama K, Aramaki T, Hara R, Kimura T, Nakamura O, Kudo M. Phase I/II study of first-line combination therapy with sorafenib plus resminostat, an oral HDAC inhibitor, versus sorafenib monotherapy for advanced hepatocellular carcinoma in east Asian patients. Invest New Drugs. 2018 Dec;36(6):1072-1084. doi: 10.1007/s10637-018-0658-x. Epub 2018 Sep 10. PMID: 30198057. 13: Dar GN, Tak SR, Kangoo KA, Halwai MA. Bridge plate osteosynthesis using dynamic condylar screw (DCS) or retrograde intramedullary supracondylar nail (RIMSN) in the treatment of distal femoral fractures: comparison of two methods in a prospective randomized study. Ulus Travma Acil Cerrahi Derg. 2009 Mar;15(2):148-53. PMID: 19353317.