OX-201
OX-201 is an orally active, blood-brain barrier-permeable OX2R agonist with an EC50 of 8.0 nM. OX-201 activates OX2R to induce wakefulness and neuronal activation. OX-201 promotes the release of neuron activity-dependent tau protein from neurons into the interstitial fluid of hippocampal tissues. OX-201 is applicable to research related to Alzheimer's disease and tauopathies.
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- No. CAS: 2460722-03-4
- Fòrmula: C22H23F5N2O4S
- Peso molecular:506.49
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Ver todos los productos específicos de isoformas Orexin Receptor (OX Receptor)
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Actividad biológica
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OX2 Receptor 8 nM (EC50) |
OX1 Receptor 8.1 μM (EC50) |
OX-201 (8.0 nM-10 μM) is a potent, highly selective OX2R agonist with minimal off-target activity in cell-based in vitro assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
OX-201 (3-30 mg/kg; p.o.; single administration or once daily for consecutive 2 months) enhances wakefulness during the active phase in male human P301S tau transgenic mice; at the dose of 30 mg/kg, it induces neuronal activation and increases interstitial fluid (ISF) tau levels in the hippocampus, while the regimen of 30 mg/kg once daily for consecutive 2 months does not exacerbate hippocampal tau aggregation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 8-12 weeks old)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Significantly increased total wakefulness time over 6 hours post-administration during the sleep phase, with dose-dependent effects.
Showed a non-significant tendency to increase hippocampal ISF tau levels for 4.5 hours at 100 mg/kg.
Significantly increased hippocampal ISF lactate levels for 7.5 hours at 100 mg/kg.
Had no clear effect on hippocampal ISF glucose levels at 100 mg/kg.
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Animal Model:human P301S tau transgenic (Tg) (male, 7-9 months old, tauopathy model)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg (single dose wakefulness/ISF studies); 30 mg/kg (chronic 2-month tau accumulation study)
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Administration:p.o.; single dose; once daily for 2 months
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Result:Significantly increased total wakefulness time during the 6-hour window post-administration (ZT13-18) during the active phase, with no residual effect on wakefulness during the subsequent sleep phase, at 3, 10, and 30 mg/kg.
Increased hippocampal ISF tau levels for > 16.5 hours at 30 mg/kg.
Increased ISF lactate levels for >6 hours at 30 mg/kg.
Increased ISF glucose levels at 30 mg/kg.
Did not alter total hippocampal tau levels after chronic once-daily administration of 30 mg/kg for 2 months.
Chemical Information
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No. CAS 2460722-03-4
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Peso molecular 506.49
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Fòrmula C22H23F5N2O4S
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SMILES
FC1=C(C2=CC(F)=CC(F)=C2)C=CC=C1C[C@]3([H])N(C(C(O)(C)C)=O)CC(F)(F)[C@]3([H])NS(=O)(C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OX-201 Related Classifications
HY-162712 Related Classifications
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