Oveporexton
Based on 1 Customer Validation
Oveporexton (TAK-861) is an orally active and selective orexin receptor 2 (OX2R) agonist with an EC50 of 2.5 nM. Oveporexton exhibits 3000-fold selectivity for OX2R over OX1R. Oveporexton can be used for the study of hypersomnia disorders including narcolepsy.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 2460722-04-5
- Formula: C23H25F5N2O4S
- Molecular Weight:520.51
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Biological Activity
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OX2 Receptor 2.5 nM (EC50) |
OX1 Receptor 7500 nM (EC50) |
Oveporexton potently activates recombinant OX2R (EC50 of 2.5 nM) and weakly activates OX1R (EC50 of 7500 nM)[2].
Oveporexton (10-1000 nM) induces dose-dependent depolarization of the membrane potential in histaminergic neurons in the mouse tuberomammillary nucleus with an EC50 of 31.7 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Oveporexton (1 mg/kg; p.o.) significantly increases wakefulness time in cynomolgus monkeys[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (3 weeks old for slice electrophysiology), male OX2R KO mice (18 weeks old), male orexin/ataxin-3 mice and their WT littermates (22-29 weeks old)[2]
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Dosage:For WT mice: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg; For OX2R KO mice: 10 mg/kg; For orexin/ataxin-3 mice: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
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Administration:Oral administration; single dose for most experiments, except for the repeated administration study in orexin/ataxin-3 mice where it was administered once daily for 14 days in the sub-chronic treatment group
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Result:Increased total wakefulness time and decreased NREM and REM sleep times (in WT mice).
Had no effect on sleep-wake parameters (in OX2R KO mice).
Increased wakefulness, decreased NREM sleep, improved wakefulness fragmentation, and reduced cataplexy -like episodes (in orexin/ataxin-3 mice).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2460722-04-5
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Appearance Solid
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Molecular Weight 520.51
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Formula C23H25F5N2O4S
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Color White to off-white
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SMILES
CC(C)(O)C(N(CC(F)([C@@H]1NS(CC)(=O)=O)F)[C@H]1CC2=C(C(C3=CC(F)=CC(F)=C3)=CC=C2)F)=O
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Synonyms
TAK-861
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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
DMSO : 50 mg/mL (96.06 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (9.61 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (9.61 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 1.9212 mL | 9.6060 mL | 19.2119 mL | 48.0298 mL |
| 5 mM | 0.3842 mL | 1.9212 mL | 3.8424 mL | 9.6060 mL | |
| 10 mM | 0.1921 mL | 0.9606 mL | 1.9212 mL | 4.8030 mL | |
| 15 mM | 0.1281 mL | 0.6404 mL | 1.2808 mL | 3.2020 mL | |
| 20 mM | 0.0961 mL | 0.4803 mL | 0.9606 mL | 2.4015 mL | |
| 25 mM | 0.0768 mL | 0.3842 mL | 0.7685 mL | 1.9212 mL | |
| 30 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6010 mL | |
| 40 mM | 0.0480 mL | 0.2401 mL | 0.4803 mL | 1.2007 mL | |
| 50 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9606 mL | |
| 60 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL | |
| 80 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6004 mL |
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