GSK1059865
Based on 1 Customer Validation
GSK1059865 is a potent orexin 1 receptor antagonist.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 1191044-58-2
- Formula: C20H23BrFN3O2
- Molecular Weight:436.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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All Orexin Receptor (OX Receptor) Isoforms
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Biological Activity
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OX1 Receptor |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1191044-58-2
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Appearance Solid
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Molecular Weight 436.32
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Formula C20H23BrFN3O2
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Color White to off-white
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SMILES
O=C(N1[C@H](CNC2=NC=C(Br)C=C2)CC[C@H](C)C1)C3=CC=CC(F)=C3OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 200 mg/mL (458.38 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Protocol
Rats: GSK1059865 is dissolved in 0.5% HPMC (w/v) in distilled water and administered by gavage at doses of 10 and 30 mg/kg to rats. Drug or vehicle is administered 1 h before access to highly palatable food[2].
Mice: During baseline and the first 5 test cycles following chronic intermittent ethanol (or air) exposure, mice receive vehicle (saline) injections (i.p.; 0.01 ml/g body weight) 30 minutes before drinking ethanol. On test cycles 6 and 7 mice receive vehicle or GSK1059865 (10, 25, 50 mg/kg) before given access to ethanol 15% v/v (Test 6) or sucrose 5% w/v (Test 7) versus water. GSK1059865 is dissolved in saline and TWEEN 80 (0.5 % v/v) as vehicle[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 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]. Lopez MF, et al. The highly selective orexin/hypocretin 1 receptor antagonist GSK1059865 potently reduces ethanol drinking in ethanol dependent mice. Brain Res. 2016 Apr 1;1636:74-80. [Content Brief]
[2]. Piccoli L, et al. Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011. [Content Brief]
[3]. Gozzi A, et al. Differential effect of orexin-1 and CRF-1 antagonism on stress circuits: a fMRI study in the rat with the pharmacological stressor Yohimbine. Neuropsychopharmacology. 2013 Oct;38(11):2120-30. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2919 mL | 11.4595 mL | 22.9190 mL | 57.2974 mL |
| 5 mM | 0.4584 mL | 2.2919 mL | 4.5838 mL | 11.4595 mL | |
| 10 mM | 0.2292 mL | 1.1459 mL | 2.2919 mL | 5.7297 mL | |
| 15 mM | 0.1528 mL | 0.7640 mL | 1.5279 mL | 3.8198 mL | |
| 20 mM | 0.1146 mL | 0.5730 mL | 1.1459 mL | 2.8649 mL | |
| 25 mM | 0.0917 mL | 0.4584 mL | 0.9168 mL | 2.2919 mL | |
| 30 mM | 0.0764 mL | 0.3820 mL | 0.7640 mL | 1.9099 mL | |
| 40 mM | 0.0573 mL | 0.2865 mL | 0.5730 mL | 1.4324 mL | |
| 50 mM | 0.0458 mL | 0.2292 mL | 0.4584 mL | 1.1459 mL | |
| 60 mM | 0.0382 mL | 0.1910 mL | 0.3820 mL | 0.9550 mL | |
| 80 mM | 0.0286 mL | 0.1432 mL | 0.2865 mL | 0.7162 mL | |
| 100 mM | 0.0229 mL | 0.1146 mL | 0.2292 mL | 0.5730 mL |
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