MedChemExpress - Model EIPA hydrochloride - 1345839-28-2

FromMedChemExpress LLC (MCE)

EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma[1][2][3][5].

EIPA hydrochloride

MCE China：EIPA hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-101840A

CAS：1345839-28-2

Synonyms：L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride

Purity：98.31%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.

In Vitro：EIPA hydrochloride (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 hydrochloride (300 μM, 6h) enhances autophagy through NHE3 (Na+/H+-exchanger 3) in IEC-18 cells[2]. ?EIPA hydrochloride (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells[3].?EIPA hydrochloride (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn2+ entry in cerebellar granule neurons[4].?EIPA hydrochloride (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression[5].?EIPA hydrochloride (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein[7].

In Vivo：EIPA hydrochloride (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice[6].?EIPA hydrochloride (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model[7].

IC50 & Target：COX-2

References：

[1]. Dai XQ, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85. [Content Brief]

[2]. Shi H, et al. Na+/H+ Exchanger Regulates Amino Acid-Mediated Autophagy in Intestinal Epithelial Cells. Cell Physiol Biochem. 2017;42(6):2418-2429. [Content Brief]

[3]. Zhu BY, et al. A new HDAC inhibitor cinnamoylphenazine shows antitumor activity in association with intensive macropinocytosis. [Content Brief]

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