Aminaftone

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Aminaftone 是 4-氨基苯甲酸的衍生物，通过干扰 pre-pro-ET-1 基因转录，而下调内皮素-1 (ET-1) 产生。

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.

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.

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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GPCR/G Protein

Endothelin Receptor

Endothelin Receptor

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14748-94-8

309.32

C18H15NO4

>98% (HPLC)

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OC=1C2=C(C(O)=C(C)C1OC(=O)C3=CC=C(N)C=C3)C=CC=C2

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(-20℃)

With Ice Pack

≥ 2 years