WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 561856
CAS#: Daridorexant mesylate
Description: Daridorexant, also known as Nemorexant and ACT541468, is a new dual orexin receptor antagonist, used in the treatment of Insomnia Disorder in Adult Patients. By specific binding to both orexin receptors, daridorexant inhibits the actions of the wake-promoting orexin (also called hypocretin) neuropeptides. This mechanism avoids a more widespread inhibition of neuronal pathways and associated side effects that are intrinsic to positive allosteric GABA-A receptor modulators.
MedKoo Cat#: 561856
Name: Daridorexant mesylate
CAS#: Daridorexant mesylate
Chemical Formula: C24H27ClN6O5S
Exact Mass:
Molecular Weight: 547.03
Elemental Analysis: C, 52.70; H, 4.98; Cl, 6.48; N, 15.36; O, 14.62; S, 5.86
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 1792993-84-0 (HCl) 1505484-82-1 (free base) Daridorexant mesylate
Synonym: Daridorexant; Daridorexant hydrochloride; Daridorexant HCl; ACT541468; ACT 541468; ACT-541468; Nemorexant;
IUPAC/Chemical Name: Methanone, ((2S)-2-(6-chloro-7-methyl-1H-benzimidazol-2-yl)-2-methyl-1-pyrrolidinyl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)-, mesylate
InChi Key: VMOSCTOMUNHUKN-BQAIUKQQSA-N
InChi Code: InChI=1S/C23H23ClN6O2.CH4O3S/c1-14-17(24)6-7-18-20(14)28-22(27-18)23(2)9-4-12-29(23)21(31)16-13-15(32-3)5-8-19(16)30-25-10-11-26-30;1-5(2,3)4/h5-8,10-11,13H,4,9,12H2,1-3H3,(H,27,28);1H3,(H,2,3,4)/t23-;/m0./s1
SMILES Code: O=C(N1[C@](C)(C2=NC3=CC=C(Cl)C(C)=C3N2)CCC1)C4=CC(OC)=CC=C4N5N=CC=N5.OS(=O)(C)=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
The following data is based on the product molecular weight 547.03 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: Ufer M, Kelsh D, Schoedel KA, Dingemanse J. Abuse potential assessment of the new dual orexin receptor antagonist daridorexant in recreational sedative drug users as compared to suvorexant and zolpidem. Sleep. 2021 Sep 4:zsab224. doi: 10.1093/sleep/zsab224. Epub ahead of print. PMID: 34480579.
2: Roch C, Bergamini G, Steiner MA, Clozel M. Nonclinical pharmacology of daridorexant: a new dual orexin receptor antagonist for the treatment of insomnia. Psychopharmacology (Berl). 2021 Oct;238(10):2693-2708. doi: 10.1007/s00213-021-05954-0. Epub 2021 Aug 20. PMID: 34415378; PMCID: PMC8455402.
3: Gehin M, Wierdak J, Sabattini G, Sidharta PN, Dingemanse J. Effect of gastric pH and of a moderate CYP3A4 inducer on the pharmacokinetics of daridorexant, a dual orexin receptor antagonist. Br J Clin Pharmacol. 2021 Aug 9. doi: 10.1111/bcp.15029. Epub ahead of print. PMID: 34371524.
4: Schilling U, Henrich A, Muehlan C, Krause A, Dingemanse J, Ufer M. Impact of Daridorexant, a Dual Orexin Receptor Antagonist, on Cardiac Repolarization Following Bedtime Dosing: Results from a Thorough QT Study Using Concentration- QT Analysis. Clin Drug Investig. 2021 Aug;41(8):711-721. doi: 10.1007/s40261-021-01062-1. Epub 2021 Jul 31. PMID: 34331678.
5: Berger B, Muehlan C, Klein G, Dingemanse J. Pharmacokinetics of daridorexant, a dual orexin receptor antagonist, are not affected by renal impairment. Clin Transl Sci. 2021 Nov;14(6):2132-2138. doi: 10.1111/cts.13079. Epub 2021 Jun 21. PMID: 34121345; PMCID: PMC8604215.
6: Berger B, Kornberger R, Dingemanse J. Pharmacokinetic and pharmacodynamic interactions between daridorexant, a dual orexin receptor antagonist, and citalopram in healthy subjects. Eur Neuropsychopharmacol. 2021 Oct;51:90-104. doi: 10.1016/j.euroneuro.2021.05.005. Epub 2021 Jun 5. PMID: 34098518.
7: Berger B, Dingemanse J, Sabattini G, Delahaye S, Duthaler U, Muehlan C, Krähenbühl S. Effect of Liver Cirrhosis on the Pharmacokinetics, Metabolism, and Tolerability of Daridorexant, A Novel Dual Orexin Receptor Antagonist. Clin Pharmacokinet. 2021 Oct;60(10):1349-1360. doi: 10.1007/s40262-021-01028-8. Epub 2021 May 18. PMID: 34002356.
8: Erratum to "Daridorexant, a New Dual Orexin Receptor Antagonist to Treat Insomnia Disorder". Ann Neurol. 2020 Sep;88(3):647-651. doi: 10.1002/ana.25801. Epub 2020 Jul 1. Erratum for: Ann Neurol. 2020 Mar;87(3):347-356. PMID: 33464656.
9: Boof ML, Dingemanse J, Brunke M, Esselmann A, Heymer P, Kestermann O, Lederer K, Fietze I, Ufer M. Effect of the novel dual orexin receptor antagonist daridorexant on night-time respiratory function and sleep in patients with moderate chronic obstructive pulmonary disease. J Sleep Res. 2021 Aug;30(4):e13248. doi: 10.1111/jsr.13248. Epub 2021 Jan 8. PMID: 33417730.
10: Boof ML, Dingemanse J, Lederer K, Fietze I, Ufer M. Effect of the new dual orexin receptor antagonist daridorexant on nighttime respiratory function and sleep in patients with mild and moderate obstructive sleep apnea. Sleep. 2021 Jun 11;44(6):zsaa275. doi: 10.1093/sleep/zsaa275. PMID: 33305817.
11: Berger B, Brooks S, Zuiker R, Richard M, Muehlan C, Dingemanse J. Pharmacological Interactions between the Dual Orexin Receptor Antagonist Daridorexant and Ethanol in a Double-Blind, Randomized, Placebo-Controlled, Double-Dummy, Four-Way Crossover Phase I Study in Healthy Subjects. CNS Drugs. 2020 Dec;34(12):1253-1266. doi: 10.1007/s40263-020-00768-8. Epub 2020 Nov 18. PMID: 33205362.
12: Boss C, Gatfield J, Brotschi C, Heidmann B, Sifferlen T, von Raumer M, Schmidt G, Williams JT, Treiber A, Roch C. The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders. ChemMedChem. 2020 Dec 3;15(23):2286-2305. doi: 10.1002/cmdc.202000453. Epub 2020 Oct 28. PMID: 32937014.
13: Muehlan C, Vaillant C, Zenklusen I, Kraehenbuehl S, Dingemanse J. Clinical pharmacology, efficacy, and safety of orexin receptor antagonists for the treatment of insomnia disorders. Expert Opin Drug Metab Toxicol. 2020 Nov;16(11):1063-1078. doi: 10.1080/17425255.2020.1817380. Epub 2020 Oct 4. PMID: 32901578.
14: Boss C. 20 Years of Medicinal Chemistry - Always Look at the Bright Side (of Life). Chimia (Aarau). 2020 Aug 12;74(7):549-560. doi: 10.2533/chimia.2020.549. PMID: 32778207.
15: Zenklusen I, Muehlan C, Ulc I, Liška J, Dingemanse J. The dual orexin receptor antagonist daridorexant does not affect the pharmacokinetics of the BCRP substrate rosuvastatin. Clin Exp Pharmacol Physiol. 2020 Nov;47(11):1843-1849. doi: 10.1111/1440-1681.13370. Epub 2020 Jul 21. PMID: 32603512.
16: Molano JRV. Daridorexant: A new medication for insomnia in older adults? Neurology. 2020 May 26;94(21):e2287-e2289. doi: 10.1212/WNL.0000000000009489. PMID: 32451342.
17: Zammit G, Dauvilliers Y, Pain S, Sebök Kinter D, Mansour Y, Kunz D. Daridorexant, a new dual orexin receptor antagonist, in elderly subjects with insomnia disorder. Neurology. 2020 May 26;94(21):e2222-e2232. doi: 10.1212/WNL.0000000000009475. Epub 2020 Apr 27. PMID: 32341187.
18: Muehlan C, Zuiker R, Peeters P, Rowles R, Dingemanse J. Pharmacokinetics and Pharmacodynamics of the Dual Orexin Receptor Antagonist Daridorexant in Japanese and Caucasian Subjects. J Clin Psychopharmacol. 2020 Mar/Apr;40(2):157-166. doi: 10.1097/JCP.0000000000001182. PMID: 32134851.
19: Dauvilliers Y, Zammit G, Fietze I, Mayleben D, Seboek Kinter D, Pain S, Hedner J. Daridorexant, a New Dual Orexin Receptor Antagonist to Treat Insomnia Disorder. Ann Neurol. 2020 Mar;87(3):347-356. doi: 10.1002/ana.25680. Epub 2020 Feb 5. Erratum in: Ann Neurol. 2020 Sep;88(3):647-651. PMID: 31953863.
20: Muehlan C, Boehler M, Brooks S, Zuiker R, van Gerven J, Dingemanse J. Clinical pharmacology of the dual orexin receptor antagonist ACT-541468 in elderly subjects: Exploration of pharmacokinetics, pharmacodynamics and tolerability following single-dose morning and repeated-dose evening administration. J Psychopharmacol. 2020 Mar;34(3):326-335. doi: 10.1177/0269881119882854. Epub 2019 Oct 23. PMID: 31642731.
