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14748-94-8

中文名稱 AMINAFTONE
英文名稱 1,4-dihydroxy-3-methyl-2-naphthyl 4-aminobenzoate
CAS 14748-94-8
分子式 C18H15NO4
分子量 309.32
MOL 文件 14748-94-8.mol
14748-94-8 結(jié)構(gòu)式 14748-94-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T14219
1,4-二羥基-3-甲基-2-萘基4-氨基苯甲酸酯
英文別名
Menatriol
Capilarema
Aminaftone
Capillarema
Aminaphthone
Einecs 238-809-8
1,4-dihydroxy-3-methyl-2-naphthyl 4-aminobenzoate
3-Methyl-1,2,4-naphthalenetriol-2-(4-aminobenzoate)
1,2,4-Naphthalenetriol, 3-methyl-, 2-(4-aminobenzoate)
4-Aminobenzoic acid 1,4-dihydroxy-3-methylnaphthalen-2-yl ester

物理化學性質(zhì)

沸點617.1±55.0 °C(Predicted)
密度1.390±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)8.00±0.50(Predicted)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS09
警示詞警告
危險性描述H400
防范說明P273-P391-P501

常見問題列表

生物活性
Aminaftone 是 4-氨基苯甲酸的衍生物,通過干擾 pre-pro-ET-1 基因轉(zhuǎn)錄,而下調(diào)內(nèi)皮素-1 (ET-1) 產(chǎn)生。
靶點

endothelin-1 (ET-1)

體外研究

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.

體內(nèi)研究

The rats are randomly assigned to the following experimental groups: Control; Monocrotaline; Aminaftone 30 mg/kg/day; Aminaftone 150 mg/kg/day. After 5 weeks, mortality is significantly lower in the animals treated with Aminaftone at both doses compared to Monocrotaline alone. Aminaftone reduces plasma concentration of ET-1 and seems to reduce right heart hypertrophy and the wall thickness of the pulmonary arteries at the highest dose. At the end of the experiment, no rats die in the control and Aminaftone 150 groups, while mortality is 38% in the Monocrotaline group and 13% in the Aminaftone 30 group. Overall, Aminaftone treated rats have a significantly lower mortality compared to rats in the Monocrotaline group (P=0.044).

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