Ledasorexton
Ledasorexton is an orally active OX2R agonist (EC50: 0.99 nM). Ledasorexton has awakening effect in mice. Ledasorexton can be used for research of neurological disease.
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。
- CAS 番号: 2758363-88-9
- 分子式: C22H32FN5O2
- 分子量:417.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
製品説明
IC50 & Target
[1]|
OX2 Receptor 0.99 nM (EC50) |
OX1 Receptor >100 nM (EC50) |
体外実験
Ledasorexton (Example 1) exhibits potent agonist activity against hOX2R with an EC50 of 0.99 nM, while showing weak activity against hOX1R (EC50 > 100 nM) in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
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 Tg mice (10-14 weeks old)[1]
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Dosage:0.3, 1, and 3 mg/kg
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Administration:i.g., single dose
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Result:Significantly prolonged sleep latency at 1 and 3 mg/kg.
Significantly suppressed cataplexy-like symptoms at 3 mg/kg.
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Animal Model:Male wild-type (WT) C57BL/6 mice (13 weeks old)[1]
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Dosage:1, 3 and 10 mg/kg
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Administration:i.g., single dose
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Result:Significantly increased spontaneous activity in mice.
Significantly increased sleep latency at 3 or 10 mg/kg.
化学情報
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CAS 番号 2758363-88-9
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分子量 417.52
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分子式 C22H32FN5O2
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SMILES
NC([C@@H](C1CC1)N2[C@@]3([H])C[C@]([C@]4([H])[C@@H](CN(C5=NC=C(F)C=N5)CC4)OC)([H])C[C@]2([H])CC3)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)