EIPA 是一种有效的TRPP3 channel抑制剂,IC50为 10.5 μM。EIPA 对Na+/H+交换 (NHE) 和巨噬细胞也有抑制作用。
产品描述
EIPA (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
体外活性
It is found that EIPA, benzamil, and phenamil rapidly and reversibly block Ca2+-activated TRPP3 channel activation at -50 mV, with IC50s of 143, 10.5, 1.1, and 0.14 μM, respectively[1]. The number of autophagic vacuoles increases dramatically in the HAE and HPE groups after EIPA treatment compares with the HAN and HPN groups. EIPA regulates the initiation and maturation of the autophagy associated with amino acids in IEC-18 cells [2]. In addition, the uptake of cinnamoylphenazine (CA-PZ) and neutral red (NR) is inhibited by EIPA [3].
细胞实验
The effect of EIPA alone (without alanine or proline) is also examined in both control (DMEM cultured cells) and amino acid-starved cells. The cells are incubated for 6 h in DMEM containing 5% FBS and either 0 or 0.3 mM EIPA (labeled QNN and QNE, respectively), HBSS containing either 0 or 0.3 mM EIPA (labeled HNN and HNE, respectively), HBSS with 1.0 mM alanine (labeled HAN) or 0.5 mM proline (labeled HPN), HBSS with 1.0 mM alanine and 0.3 mM EIPA (labeled HAE), and HBSS with 0.5 mM proline and 0.3 mM EIPA (labeled HPE) [2].
Cas No.
1154-25-2
分子式
C11H18ClN7O
分子量
299.76
别名
MH 12-43;L593754
储存和溶解度
DMSO:135 mg/mL (450.36 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years