| Bioactivity | 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][5]. | |||||||||
| Invitro | 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]. Cell Proliferation Assay[5] Cell Line: | |||||||||
| 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]. Animal Model: | |||||||||
| Name | EIPA | |||||||||
| CAS | 1154-25-2 | |||||||||
| Formula | C11H18ClN7O | |||||||||
| Molar Mass | 299.76 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Dai XQ, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85. [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. [3]. Zhu BY, et al. A new HDAC inhibitor cinnamoylphenazine shows antitumor activity in association with intensive macropinocytosis. [4]. E V Stelmashook, et al. Acidosis and 5-(N-ethyl-N-isopropyl)amiloride (EIPA) Attenuate Zinc/Kainate Toxicity in Cultured Cerebellar Granule Neurons. Biochemistry (Mosc). 2015 Aug;80(8):1065-72. [5]. Shigekuni Hosogi, et al. An inhibitor of Na(+)/H(+) exchanger (NHE), ethyl-isopropyl amiloride (EIPA), diminishes proliferation of MKN28 human gastric cancer cells by decreasing the cytosolic Cl(-) concentration via DIDS-sensitive pathways. Cell Physiol Biochem. 2012;30(5):1241-53. [6]. Junji Yamashita, et al. Role of Na+/H+ exchanger in the pathogenesis of ischemic acute renal failure in mice. J Cardiovasc Pharmacol. 2007 Mar;49(3):154-60. [7]. Fumitaka Kamachi, et al. Inhibition of lipopolysaccharide-induced prostaglandin E2 production and inflammation by the Na+/H+ exchanger inhibitors. J Pharmacol Exp Ther. 2007 Apr;321(1):345-52. |