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.
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- Pureté: 99.94%
- CAS No.: 2861934-86-1
- Formule: C22H25F3N2O4S.3/2H2O
- Masse moléculaire:497.53
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Stockage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Voir tous les produits spécifiques à Isoform Orexin Receptor (OX Receptor)
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Activité biologique
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OX2 Receptor |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2861934-86-1
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Appearance Solid
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Masse moléculaire 497.53
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureté et documentation
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Fiche technique (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)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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