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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.94%
- CAS 番号: 2861934-86-1
- 分子式: C22H25F3N2O4S.3/2H2O
- 分子量:497.53
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保管条件:
-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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Orexin Receptor (OX Receptor) アイソフォーム固有の製品をすべて表示
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生物活性
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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 |
化学情報
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CAS 番号 2861934-86-1
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性状 Solid
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分子量 497.53
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分子式 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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別名
TAK-994
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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