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.
For research use only. We do not sell to patients.
- CAS No.: 2460722-03-4
- Formula: C22H23F5N2O4S
- Molecular Weight:506.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Orexin Receptor (OX Receptor) Isoforms
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Biological Activity
Description
IC50 & Target
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OX2 Receptor 8 nM (EC50) |
OX1 Receptor 8.1 μM (EC50) |
In Vitro
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. Further protocols information, click here.
In Vivo
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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CAS No. 2460722-03-4
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Molecular Weight 506.49
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OX-201 Related Classifications
HY-162712 Related Classifications
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