EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC 50 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.
性状
Solid
IC50 & Target[1][2]
COX-2
体外研究(In Vitro)
EIPA hydrochloride (100 μM, 30 min) suppresses TRPP3-mediated Ca uptake in X. laevis oocytes .EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na current (IC50: 19.5 μM).EIPA hydrochloride (300 μM, 6h) enhances autophagy through NHE3 (Na/H-exchanger 3) in IEC-18 cells. EIPA hydrochloride (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells.EIPA hydrochloride (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn entry in cerebellar granule neurons.EIPA hydrochloride (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression.EIPA hydrochloride (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein. has not independently confirmed the accur
体内研究(In Vivo)
EIPA hydrochloride (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice.
EIPA hydrochloride (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[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 cinnamoylphena
溶解度数据
In Vitro: DMSO : 130 mg/mL (386.65 mM; Need ultrasonic)配制储备液