Danavorexton
Based on 1 Customer Validation
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.56%
- CAS 番号: 2114324-48-8
- 分子式: C21H32N2O5S
- 分子量:424.55
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Orexin Receptor (OX Receptor) アイソフォーム固有の製品をすべて表示
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生物活性
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Common marmosets and cynomolgus monkeys models[2]
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Dosage:1, 10 mg/kg (1, 3 mg/kg)
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Administration:s.c.
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Result:Decreased SWS I (Sleeping With Sirens I), SWS II (Sleeping With Sirens II) and REM (Rapid Eye Movement) sleep time.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2114324-48-8
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性状 Solid
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分子量 424.55
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分子式 C21H32N2O5S
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Color White to off-white
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SMILES
O=C(N1[C@@H](CO[C@H]2CC[C@@H](C3=CC=CC=C3)CC2)[C@@H](NS(=O)(C)=O)CCC1)OC
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別名
TAK-925
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : ≥ 50 mg/mL (117.77 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC/saline water
Solubility: 12.5 mg/mL (29.44 mM); Clear solution; Need ultrasonic
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Evans R, et al. 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 [Content Brief]
[3]. Ishikawa T, et al. Danavorexton, a selective orexin 2 receptor agonist, provides a symptomatic improvement in a narcolepsy mouse model. Pharmacol Biochem Behav. 2022 Oct;220:173464. [Content Brief]
[4]. Fujimoto T, et al. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3554 mL | 11.7772 mL | 23.5544 mL | 58.8859 mL |
| 5 mM | 0.4711 mL | 2.3554 mL | 4.7109 mL | 11.7772 mL | |
| 10 mM | 0.2355 mL | 1.1777 mL | 2.3554 mL | 5.8886 mL | |
| 15 mM | 0.1570 mL | 0.7851 mL | 1.5703 mL | 3.9257 mL | |
| 20 mM | 0.1178 mL | 0.5889 mL | 1.1777 mL | 2.9443 mL | |
| 25 mM | 0.0942 mL | 0.4711 mL | 0.9422 mL | 2.3554 mL | |
| 30 mM | 0.0785 mL | 0.3926 mL | 0.7851 mL | 1.9629 mL | |
| 40 mM | 0.0589 mL | 0.2944 mL | 0.5889 mL | 1.4721 mL | |
| 50 mM | 0.0471 mL | 0.2355 mL | 0.4711 mL | 1.1777 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9814 mL | |
| 80 mM | 0.0294 mL | 0.1472 mL | 0.2944 mL | 0.7361 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2355 mL | 0.5889 mL |