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);3-氨基-N-氨基甲酰基-6-氯-5-(乙基(异丙基)氨基)吡嗪-2-甲酰胺;A盐酸盐;5-(N-乙基-N-异丙基)阿米洛利(EIPA) |
| 英文名称 | EIPA |
| 英文同义词 | AMILORIDE, 5-(N-ETHYL-N-ISOPROPYL)-;5-(N-ETHYL-N-ISOPROPYL)AMILORIDE;3-AMINO-N-(AMINOIMINOMETHYL)-6-CHLORO-5-[ETHYL(2-PROPYL)AMINO]-PYRAZINE-2-CARBOXAMIDE;EIPA;3-Amino-N-(aminoiminomethyl)-6-chloro-5-[ethyl(1-methylethyl)amino]-2-pyrazinecarboxamide;L 593754;MH 12-43;3-Amino-5-(N-ethyl-N-isopropylamino)-6-chloro-N-(aminoiminomethyl)-2-pyrazinecarboxamide |
| 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 |
| 结构式 |  |
5-(N-乙基-N-异丙基)阿米洛利 性质
| 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 |
| 溶解度 | 可溶于乙腈（轻微加热）、DMSO（轻微）、甲醇（轻微） |
| 酸度系数(pKa) | 8.67±0.46(Predicted) |
| 形态 | 灰白色至黄色固体。 |
| 颜色 | 淡黄色至绿色 |
| 稳定性 | 在甲醇中不稳定 |
| CAS 数据库 | 1154-25-2 |
IC50: 10.5 μM (TRPP3 channel)
NHE
Macropinocytosis
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.
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