EIPA

EIPA (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM) . It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.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. 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. In addition, the uptake of cinnamoylphenazine (CA-PZ) and neutral red (NR) is inhibited by EIPA. (In Vitro) :EIPA (100 μM, 30 min) suppresses TRPP3-mediated Ca2+ uptake in X. laevis oocytes. EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na+ current (IC50: 19.5 μM) . EIPA (300 μM, 6h) enhances autophagy through NHE3 (Na+/H+-exchanger 3) in IEC-18 cells. EIPA (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells. EIPA (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn2+ entry in cerebellar granule neurons. EIPA (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression. EIPA (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein. (In Vivo) :EIPA (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion) -induced renal dysfunction in ddY strain mice.EIPA (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model.