2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor) Tau Protein
  4. 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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OX-201

OX-201 Chemical Structure

CAS No. : 2460722-03-4

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OX-201 Related Antibodies

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Description

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[1].

IC50 & Target

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.

OX-201 Related Antibodies
In Vivo

OX-201 (10-100 mg/kg; p.o.; single administration) exerts a potent, dose-dependent arousal-promoting effect in healthy male C57BL/6J mice[1].
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.

Animal Model: C57BL/6J (male, 8-12 weeks old)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; single dose
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.
Animal Model: human P301S tau transgenic (Tg) (male, 7-9 months old, tauopathy model)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg (single dose wakefulness/ISF studies); 30 mg/kg (chronic 2-month tau accumulation study)
Administration: p.o.; single dose; once daily for 2 months
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.
Molecular Weight

506.49

Formula

C22H23F5N2O4S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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OX-201 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OX-2012460722-03-4OX201OX 201Orexin Receptor (OX Receptor)Tau ProteinHypocretin ReceptorHCRT Receptorhippocampal ISF tauOX2Rhuman P301S tau transgenic miceC57BL/6J micealzheimer's diseaseneuronal activationhippocampal tau levelstauopathyhippocampal interstitial fluidneuronsInhibitorinhibitorinhibit

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