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.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1354039-86-3
- Formula: C31H38N2O5
- Molecular Weight:518.64
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Orexin Receptor (OX Receptor) Isoforms
More
Biological Activity
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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.
Chemical Information
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CAS No. 1354039-86-3
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Appearance Solid
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Molecular Weight 518.64
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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 |
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