EIPA

EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA also enhances autophagy by inhibiting Na⁺/H⁺-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma^{[1][2][3][4][5][6][7]}. IC50 & Target:IC50: 10.5 μM (TRPP3)^[1]
NHE^[2]
Macropinocytosis^[3]
In Vitro: EIPA (100 μM, 30 min) suppresses TRPP3-mediated Ca²⁺ uptake in X. laevis oocytes^[1].
EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na⁺ current (IC₅₀: 19.5 μM)^[1].
EIPA (300 μM, 6h) enhances autophagy through NHE3 (Na⁺/H⁺-exchanger 3) in IEC-18 cells^[2].
EIPA (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells^[3].
EIPA (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn²⁺ entry in cerebellar granule neurons^[4].
EIPA (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression^[5].
EIPA (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein^[7]. In Vivo: EIPA (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice^[6].
EIPA (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model^[7].