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  2. GPCR/G Protein Neuronal Signaling MAPK/ERK Pathway Stem Cell/Wnt
  3. Orexin Receptor (OX Receptor) ERK
  4. Firazorexton hydrate

Firazorexton hydrate  (Synonyms: TAK-994)

目錄號(hào): HY-137440A 純度: 99.94%
COA 產(chǎn)品使用指南 技術(shù)支持

Firazorexton hydrate (TAK-994) 是一種具有口服活性、腦滲透性的食欲素 2 型受體 (OX2R) 選擇性激動(dòng)劑。Firazorexton hydrate (TAK-994) 能夠促進(jìn)小鼠覺醒，具有改善嗜睡病樣癥狀的潛力。

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Firazorexton hydrate Chemical Structure

Firazorexton hydrate Chemical Structure

CAS No. : 2861934-86-1

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1 mg ￥4875
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Other Forms of Firazorexton hydrate:

查看 Orexin Receptor (OX Receptor) 亞型特異性產(chǎn)品:

查看 ERK 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

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[1].

IC50 & Target[1]

OX2 Receptor

 

體外研究
(In Vitro)

Firazorexton (hydrate) (1-1000 nM) 以劑量依賴性的方式增加 hOX2R/CHO-K1 細(xì)胞中的鈣動(dòng)員，EC50 為 19 nM[1]。
Firazorexton (hydrate) (1 nM-10 μM) 在 hOX2R/CHO-EA 細(xì)胞中激活 OX2R 下游信號(hào)，增加 β-arrestin 的招募 (EC50 : 100 nM)，誘導(dǎo) ERK1/2 的磷酸化 (EC50 : 170 nM)[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Firazorexton (hydrate) (口服; 30 mg/kg; 單劑量 ) 可增加 C57BL/6J 小鼠的總覺醒時(shí)間[1]。
Firazorexton (hydrate) (口服; 3-10 mg/kg; 單劑量) 可改善嗜睡癥小鼠模型中發(fā)作性睡病樣癥狀[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Orexin/ataxin-3 mice model[1]
Dosage: 3 and 10 mg/kg
Administration: Oral administration (p.o.); single dose
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.
Clinical Trial
分子量

497.53

Formula

C22H25F3N2O4S.3/2H2O
CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

純度 & 產(chǎn)品資料

純度: 99.94%

參考文獻(xiàn)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

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產(chǎn)品名稱：
Firazorexton hydrate
目錄號(hào)：
HY-137440A
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