| Identification | Back Directory | [Name]
RO5263397 | [CAS]
1357266-05-7 | [Synonyms]
RO5263397
(S)-4-(3-FLUORO-2-METHYLPHENYL)-4,5-DIHYDROOXAZOL-2-AMINE | [Molecular Formula]
C10H11FN2O | [MDL Number]
MFCD28405323 | [MOL File]
1357266-05-7.mol | [Molecular Weight]
194.21 |
| Chemical Properties | Back Directory | [Boiling point ]
303.9±52.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO : 260 mg/mL (1338.76 mM; Need ultrasonic) | [form ]
powder | [pka]
7.68±0.70(Predicted) | [color ]
white to beige | [Optical Rotation]
[α]/D +77 to +88°, c = 1.0 in methanol |
| Hazard Information | Back Directory | [Uses]
RO 5263397 is a trace amine-associated receptor 1 agonist (TAAR1). | [Biological Activity]
RO5256390 is an orally available partial agonist th at targets trace amine-associated receptor 1 (TAAR1) with high affinity (Ki in nM = 0.9/mouse4.1/human9.1/rat24/monkey TARR1)potency (EC50 in nM/relative efficacy with respect to β-phenylethylamine = 1.3/0.59/mouse17/0.81/human47/0.76/rat251/0.85/monkey TARR1-dependent cellular cAMP production)and selectivity (by a 112-receptor/channel/transporter and a 42-enzyme panel)without agonistic activity toward mouse TAAR4-expressing cells even at a high concentration of 30 μM. When applied via oral administration (0.003-1 mg/kg)RO5256390 exhibits similar in vivo efficacy as the full agonist RO5256390 in blocking psychostimulants-induced hyperlocomotion in mice. | [in vivo]
RO5263397 (0.1-1.0?mg/kg; p.o.; dosing at the mid-light phase (ZT6)) increases 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]. | 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 |
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| Company Name: |
Twochem Co.Ltd
|
| Tel: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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