5-(N-乙基-N-异丙基)阿米洛利

中文名称:

5-(N-乙基-N-异丙基)阿米洛利

中文同义词:

5-(N-乙基-N-异丙基)阿米洛利;TRPP3CHANNEL抑制剂(EIPA)

英文名称:

EIPA

英文同义词:

AMILORIDE, 5-(N-ETHYL-N-ISOPROPYL)-;Amiloride,5-(N-Ethyl-N-isopropyl)-[5-(N-Ethyl-N-isopropyl)amiloride;5-(N-ETHYL-N-ISOPROPYL)AMILORIDE;3-AMINO-N-(AMINOIMINOMETHYL)-6-CHLORO-5-[ETHYL(2-PROPYL)AMINO]-PYRAZINE-2-CARBOXAMIDE;ethylisopropylamiloride;EIPA;3-Amino-N-(aminoiminomethyl)-6-chloro-5-[ethyl(1-methylethyl)amino]-2-pyrazinecarboxamide;L 593754

CAS号:

1154-25-2

分子式:

C11H18ClN7O

分子量:

299.76

EINECS号:

相关类别:

合成;细胞生物学试剂;All Inhibitors;Bases Related Reagents;Inhibitors;Intermediates Fine Chemicals;Nucleotides;Pharmaceuticals

Mol文件:

1154-25-2.mol

熔点 

202-205 °C(lit.)

密度 

1.49±0.1 g/cm3(Predicted)

储存条件 

Keep in dark place,Sealed in dry,2-8°C

形态

Off-white to yellow solid.

酸度系数(pKa)

8.67±0.46(Predicted)

CAS 数据库

1154-25-2

生物活性

EIPA (L593754) 是一种 TRPP3 channel 抑制剂，其 IC50 值为 10.5 μM。EIPA 还抑制 Na+/H+ 交换 (NHE) 和巨噬细胞。

靶点

IC50: 10.5 μM (TRPP3 channel) NHE Macropinocytosis

体外研究

In the presence of 100 μM EIPA, 10 μM benzamil, and 10 μM phenamil, 45 Ca 2+ uptake decreases from 79±9 to 46±4 (58% remaining), 27±4 (34%), 29±5 (37%), and 38±4 (48%) pmol/oocyte/30 min (n=6, P=0.008), respectively. It is found that EIPA, benzamil, and phenamil rapidly and reversibly block Ca 2+ -activated TRPP3 channel activation at -50 mV, with IC 50 s of 143±8 (n=36), 10.5±2.2 (n=28), 1.1±0.3 (n=30), and 0.14±0.04 μM (n=25), respectively. The number of autophagic vacuoles increases dramatically in the HAE and HPE groups after EIPA treatment compare with the HAN and HPN groups. EIPA regulates the initiation and maturation of the autophagy associated with amino acids in IEC-18 cells. In addition, the uptake of cinnamoylphenazine (CA-PZ) and neutral red (NR) is inhibited by EIPA.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26-37/39

危险品运输编号 

2811

WGK Germany 

3

HazardClass 

6.1(b)

PackingGroup 

III