[CAS NO. 1357266-05-7] RO5263397
PRODUCTS SPECIFICATIONS [1357266-05-7]
DESCRIPTION [1357266-05-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 194.21 |
| Molecular Formula | C10H11FN2O |
| SMILES | CC1=C([C@@H]2N=C(N)OC2)C=CC=C1F |
Summary
In Vivo
RO5263397 (0.1-1.0 mg/kg; p.o.; dosing at the mid-light phase (ZT6)) increased wake time at 0.3 and 1 mg/kg
[2]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Adult 4-5-month-old male WT littermates (C57BL/6 background) [2] |
| Dosage: | 0.1, 0.3, 1 mg/kg |
| Administration: | p.o.; dosing at the mid-light phase (ZT6) |
| Result: | Increased wake time at 0.3 and 1 mg/kg |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 260 mg/mL ( 1338.76 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 5.1491 mL | 25.7453 mL | 51.4907 mL |
| 5 mM | 1.0298 mL | 5.1491 mL | 10.2981 mL |
| 10 mM | 0.5149 mL | 2.5745 mL | 5.1491 mL |
References
- [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.
- [2] Schwartz MD, et al. Trace Amine-Associated Receptor 1 Regulates Wakefulness and EEG Spectral Composition.Neuropsychopharmacology. 2017 May;42(6):1305-1314.
- [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.