RO5263397
Based on 1 Customer Validation
RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.10%
- No. CAS: 1357266-05-7
- Fòrmula: C10H11FN2O
- Peso molecular:194.21
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
17 nM
Compound: 48; RO5263397
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Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
Agonist activity at human TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
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[PMID: 26985297] |
| HEK293 | EC50 |
35 nM
Compound: 48; RO5263397
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Agonist activity at rat TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
Agonist activity at rat TAAR1 expressed in recombinant HEK293 cells assessed as cAMP accumulation after 30 mins by luminometer
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[PMID: 26985297] |
? RO5263397 (0.3 and 1.0?mg/kg; p.o.) decreases NREM time in WT mice. RO5263397 (0.3 and 1.0?mg/kg; p.o.; in OE mice) powerfully increases W time in OE mice for 5-6?h. NREM sleep is suppressed for 4-6?h and REM sleep is almost completely suppressed for 6?h after all doses of RO5263397[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult 4-5-month-old male WT littermates (C57BL/6 background)[2]
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Dosage:0.1, 0.3, 1 mg/kg
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Administration:p.o.; dosing at the mid-light phase (ZT6)
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Result:Increased wake time at 0.3 and 1 mg/kg
Chemical Information
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No. CAS 1357266-05-7
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Appearance Solid
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Peso molecular 194.21
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Fòrmula C10H11FN2O
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Color White to off-white
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SMILES
CC1=C([C@@H]2N=C(N)OC2)C=CC=C1F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 260 mg/mL (1338.76 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: ≥ 6.5 mg/mL (33.47 mM); Clear solution
This protocol yields a clear solution of ≥ 6.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (65.0 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: ≥ 6.5 mg/mL (33.47 mM); Clear solution
This protocol yields a clear solution of ≥ 6.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (65.0 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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Galley G, et al. Discovery and Characterization of 2-Aminooxazolines as Highly Potent, Selective, and Orally Active TAAR1 Agonists.ACS Med Chem Lett. 2015 Dec 30;7(2):192-7. [Content Brief]
[2]. Schwartz MD, et al. Trace Amine-Associated Receptor 1 Regulates Wakefulness and EEG Spectral Composition.Neuropsychopharmacology. 2017 May;42(6):1305-1314. [Content Brief]
[3]. Espinoza S, et al. Biochemical and Functional Characterization of the Trace Amine-Associated Receptor 1 (TAAR1) Agonist RO5263397.Front Pharmacol. 2018 Jun 21;9:645. [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 | 5.1491 mL | 25.7453 mL | 51.4907 mL | 128.7266 mL |
| 5 mM | 1.0298 mL | 5.1491 mL | 10.2981 mL | 25.7453 mL | |
| 10 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL | 12.8727 mL | |
| 15 mM | 0.3433 mL | 1.7164 mL | 3.4327 mL | 8.5818 mL | |
| 20 mM | 0.2575 mL | 1.2873 mL | 2.5745 mL | 6.4363 mL | |
| 25 mM | 0.2060 mL | 1.0298 mL | 2.0596 mL | 5.1491 mL | |
| 30 mM | 0.1716 mL | 0.8582 mL | 1.7164 mL | 4.2909 mL | |
| 40 mM | 0.1287 mL | 0.6436 mL | 1.2873 mL | 3.2182 mL | |
| 50 mM | 0.1030 mL | 0.5149 mL | 1.0298 mL | 2.5745 mL | |
| 60 mM | 0.0858 mL | 0.4291 mL | 0.8582 mL | 2.1454 mL | |
| 80 mM | 0.0644 mL | 0.3218 mL | 0.6436 mL | 1.6091 mL | |
| 100 mM | 0.0515 mL | 0.2575 mL | 0.5149 mL | 1.2873 mL |
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