NSD 1034
NSD 1034 is a potent inhibitor of aromatic L-amino acid decarboxylase (AADC) and tyrosine aminotransferase (TAT), with IC50 values of 0.32 μM and 80 μM, respectively. NSD 1034 increases dopamine synthesis and release by inhibiting AADC and TAT, and stimulating tyrosine hydroxylase in dopaminergic neurons via calcium influx in a classical dopamine receptor-independent manner. NSD 1034 is used in studies of Parkinson's disease and sleep disorders.
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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: 555-62-4
- 分子式: C8H12N2O
- 分子量:152.19
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
生物活性
製品説明
IC50 & Target
[1]|
AADC 0.32 μM (IC50) |
TAT 80 μM (IC50) |
体外実験
NSD 1034 (80 μM) inhibits male Wistar rat liver tyrosine aminotransferase in vitro with an IC50 of 80 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
NSD 1034 (12.5-200 mg/kg; s.c.; single dose; treatment for 10-60 min) dose- and time-dependently increases DOPA accumulation in the striatum, cerebral hemispheres, and limbic areas, as well as 5-HTP accumulation in all tested brain regions in a rat model[1].
NSD 1034 (2-400 mg/kg; s.c.; single dose; treatment for 2-4 h) reduces p-tyramine concentrations and bidirectionally modulates m-tyramine concentrations in the striatum in an albino Swiss mouse model[3].
NSD 1034 (100 mg/kg; s.c.; single dose; during electrophysiological recording) does not alter the firing frequency of dopaminergic neurons in the substantia nigra in anesthetized rat models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 220-400 g)[1]
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Dosage:12.5 mg/kg, 25 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 107 mg/kg, 268 mg/kg
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Administration:s.c.; single dose; 10, 20, 30, 45, 60 min
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Result:Promote DOPA accumulation in the striatum and inhibit AADC activity.
Increased DOPA accumulation in the striatum, cerebral hemispheres, and limbic regions, and increased 5-HTP accumulation in all brain regions examined, in a dose- and time-dependent manner.
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Animal Model:albino Swiss mice (male, 18-22 g body weight)[3]
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Dosage:2, 20, 400 mg/kg
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Administration:s.c.; single dose; 2 or 4 h
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Result:Significantly reduced the concentration of p-tyramine in the mouse striatum at all tested doses (2, 20, 400 mg/kg).
Mildly increased the concentration of m-tyramine at lower doses (2 and 20 mg/kg), but significantly reduced the concentration of m-tyramine at the high dose (400 mg/kg).
化学情報
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CAS 番号 555-62-4
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分子量 152.19
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分子式 C8H12N2O
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SMILES
OC1=CC=CC(CN(C)N)=C1
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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.
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)
NSD 1034 関連分類
HY-187668 関連分類
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