Aminaftone
Aminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 (ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.
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- CAS 番号: 14748-94-8
- 分子式: C18H15NO4
- 分子量:309.32
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- プロトコル
- 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
endothelin-1 (ET-1)[1]
Aminaftone inhibits Endothelin-1 (ET-1) production in cell cultures by interfering with transcription of the pre-pro-endothelin-1 (PPET-1) gene. Incubation with IL-1beta increases concentrations of ET-1 and PPET-1 relative gene expression. Incubation with Aminaftone significantly reduces production of ET-1 in a concentration-dependent manner. A strong direct correlation is found between ET-1 concentrations and PPET-1 relative gene expression, but Aminaftone does not influence endothelin-converting enzyme (ECE) activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 14748-94-8
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分子量 309.32
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分子式 C18H15NO4
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SMILES
OC1=C2C=CC=CC2=C(O)C(C)=C1OC(C3=CC=C(N)C=C3)=O
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別名
Aminaftone; Aminaphthone
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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
Human ECV304 endothelial cells are incubated with interleukin-1beta (IL-1beta) 100 IU/mL with or without the addition of increasing concentrations of Aminaftone (2, 4 or 6 μg/mL). ET-1 concentrations in surnatants are quantified by enzyme immunoassay kit at 3, 6 and 12 hours. PPET-1 gene expressions are also analysed by real-time polymerase chain reaction (RT-PCR) at the same time points. ECE activity is also determined[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[2]
Male Wistar rats weighing 300±30 g are randomly assigned to one of the following four experimental groups: 1) control healthy rats (n=11); 2) only injection of Monocrotaline (n=12); 3) injection of Monocrotaline followed by Aminaftone 30 mg/kg treatment (Aminaftone30) (n=8); and 4) injection of Monocrotaline followed by Aminaftone 150 mg/kg treatment (Aminaftone150) (n=8). Aminaftone is administered as food admix. Rats are weighed twice a week.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
[1]. Scorza R, et al. Aminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 production in ECV304 Cells: an in vitro Study. Drugs R D. 2008;9(4):251-7. [Content Brief]
[2]. Zambelli V, et al. Efficacy of aminaftone in a rat model of monocrotaline-induced pulmonary hypertension. Eur J Pharmacol. 2011 Sep 30;667(1-3):287-91. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Aminaftone 関連分類
HY-19890 関連分類
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