ACT-335827
Based on 1 Customer Validation
ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders.
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: 98.0%
- CAS 番号: 1354039-86-3
- 分子式: C31H38N2O5
- 分子量:518.64
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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
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OX1 6 nM (IC50) |
OX2 417 nM (IC50) |
ACT-335827 (0-10 μM, 2 h) acts on OXR-1 and OXR-2 with the Kb values of 41 nM and 560 nM, the IC50 values of 120 nM and 2300 nM, respectively in CHO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ACT-335827 (oral administration, 300 mg/kg, everyday, 4 weeks) has less effect on metabolic syndrome (MetS), such as diet-induced obesity (DIO) in male Wistar rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:30, 100 or 300 mg/kg
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Administration:Oral gavage; once
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Result:Reduced fear-induced startle response at 300 mg/kg.
Decreased stress-induced elevated body temperature at 300 mg/kg and accelerated heat rate at 100 or 300 mg/kg but no effect on locomotion and blood pressure.
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Animal Model:Male Wistar rats weighing160-180g[2]
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Dosage:300 mg/kg
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Administration:Oral administration; everyday; 4 weeks
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Result:Reduced preference for high fat/sweet diets but no effect on absolute energy intake.
Increased water intake and HDL relative to total cholesterol.
Resulted in a 4% weight gain compared to the control group.
化学情報
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CAS 番号 1354039-86-3
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性状 Solid
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分子量 518.64
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分子式 C31H38N2O5
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Color Off-white to light yellow
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SMILES
COC1=C(OC)C=CC(C[C@H]2C3=CC(OC)=C(OC)C=C3CCN2[C@H](C4=CC=CC=C4)C(NC(C)C)=O)=C1
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
Ethanol : 51.864 mg/mL (100.00 mM; Need ultrasonic)
DMSO : 51.864 mg/mL (100.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Michel A Steiner, et al. Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist. ChemMedChem. 2013 Jun;8(6):898-903. [Content Brief]
[2]. Michel A Steiner, et al. The selective orexin receptor 1 antagonist ACT-335827 in a rat model of diet-induced obesity associated with metabolic syndrome. Front Pharmacol. 2013 Dec 30;4:165. [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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 1.9281 mL | 9.6406 mL | 19.2812 mL | 48.2030 mL |
| 5 mM | 0.3856 mL | 1.9281 mL | 3.8562 mL | 9.6406 mL | |
| 10 mM | 0.1928 mL | 0.9641 mL | 1.9281 mL | 4.8203 mL | |
| 15 mM | 0.1285 mL | 0.6427 mL | 1.2854 mL | 3.2135 mL | |
| 20 mM | 0.0964 mL | 0.4820 mL | 0.9641 mL | 2.4101 mL | |
| 25 mM | 0.0771 mL | 0.3856 mL | 0.7712 mL | 1.9281 mL | |
| 30 mM | 0.0643 mL | 0.3214 mL | 0.6427 mL | 1.6068 mL | |
| 40 mM | 0.0482 mL | 0.2410 mL | 0.4820 mL | 1.2051 mL | |
| 50 mM | 0.0386 mL | 0.1928 mL | 0.3856 mL | 0.9641 mL | |
| 60 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8034 mL | |
| 80 mM | 0.0241 mL | 0.1205 mL | 0.2410 mL | 0.6025 mL |
ACT-335827 関連分類
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