Firazorexton hydrate
Based on 1 Customer Validation
Firazorexton hydrate (TAK-994) is an orally active and brain-penetrant orexin type 2 receptor (OX2R) selective agonist. Firazorexton hydrate can promote wakefulness and has the potential to improve narcolepsy-like symptoms in mice.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.94%
- No. CAS: 2861934-86-1
- Fòrmula: C22H25F3N2O4S.3/2H2O
- Peso molecular:497.53
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas Orexin Receptor (OX Receptor)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
OX2 Receptor |
In Vitro
Firazorexton (hydrate) (1-1000 nM) increases calcium mobilization in hOX2R/CHO-K1 cells in a dose-dependent manner, with an EC50 of 19 nM[1].
Firazorexton (hydrate) (1 nM-10 μM) activates downstream signals of OX2R, increases the recruitment of β-arrestin (EC50: 100 nM), and induces the phosphorylation of ERK1/2 (EC50: 170 nM) in hOX2R/CHO-EA cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Firazorexton (hydrate) (oral administration; 3-10 mg/kg; single dose) can improve narcolepsy-like symptoms in mouse models of narcolepsy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Orexin/ataxin-3 mice model[1]
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Dosage:3 and 10 mg/kg
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Administration:Oral administration (p.o.); single dose
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Result:Significantly increased total wakefulness time.
Decreased total NREM sleep time and REM sleep time.
Significantly ameliorated fragmentation of wakefulness with fewer number of wakefulness episodes and longer mean duration of wakefulness episodes.
Significantly increased gamma power during wakefulness at dose of 10 mg/kg.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2861934-86-1
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Appearance Solid
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Peso molecular 497.53
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Fòrmula C22H25F3N2O4S.3/2H2O
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Color White to off-white
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SMILES
O=C(N(CC1)[C@H]([C@H]1N[S](C)(=O)=O)CC(C=CC=C2C3=CC(F)=CC(F)=C3)=C2F)C(C)(O)C.[1.5].O
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Synonyms
TAK-994
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Firazorexton hydrate Related Classifications
HY-137440A Related Classifications
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