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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- Purity: 99.94%
- CAS No.: 2861934-86-1
- 화학식: C22H25F3N2O4S.3/2H2O
- 분자량:497.53
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보관:
-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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Orexin Receptor (OX Receptor) Isoforms
More
Biological Activity
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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
|
|---|---|---|---|---|
| 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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분자량 497.53
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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