Daridorexant ( ACT541468 )
Daridorexant 是一种双重食欲素受体拮抗剂 (DORA)，专为治疗失眠而设计和开发。 Daridorexant 通过阻断食欲素的活动来减少与失眠相关的过度清醒。
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Daridorexant ( ACT541468 ) |
|---|---|
| Iupac 化学名称 | 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)- |
| 同义词 | Daridorexant ; ACT541468 ; ACT 541468 ; ACT-541468 |
| 英文同义词 | Daridorexant ; ACT541468 ; ACT 541468 ; ACT-541468 |
| 分子式 | C23H23ClN6O2 |
| 分子量 | 450.92 |
| Smile | O=C(N1[C@](C)(C2=NC3=CC=C(Cl)C(C)=C3N2)CCC1)C4=CC(OC)=CC=C4N5N=CC=N5 |
| InChiKey | NBGABHGMJVIVBW-QHCPKHFHSA-N |
| InChi | InChI=1S/C23H23ClN6O2/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/h5-8,10-11,13H,4,9,12H2,1-3H3,(H,27,28)/t23-/m0/s1 |
| Cas号 | 1505484-82-1 |
| 相关CAS号 | 1505484-82-1 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | ≧98.0% |
| 存储 | 0-4 ℃ 可短期保存（两周）；- 20 ℃ 可长期保存。 |
| 可溶性 | 溶于DMSO |
| 处理方式 | Refer to MSDS operation |
| 运输条件 | 可在室温下运输。 |
| 海关编码 | 2934200090 |
| Targets | dual orexin receptor antagonist (DORA) |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: 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.
2: 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.
3: 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.
4: 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.
5: 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.
6: 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. 2020 Dec 11:zsaa275. doi: 10.1093/sleep/zsaa275. Epub ahead of print. PMID: 33305817.
7: 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.
8: 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.
9: 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.
10: 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.
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