产品
编 号:F048154
分子式:C11H18ClN7O
分子量:299.76
产品类型
结构图
CAS No: 1154-25-2
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产品详情
生物活性:
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.
体内研究:
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.Animal Model:Male ddY strain mice
Dosage:1 mg/kg
Administration:Intravenous injection
Result:Attenuated histologic renal damage, and imprved the I/R-induced increases in renal ET-1 contents.
Animal Model:Air pouch-type LPS-induced inflammation model
Dosage:10 mg/kg
Administration:Oral administration
Result:Inhibited the LPS-induced infiltration of leukocytes into the pouch.Inhibited the amount of PGE2 in the pouch fluid.
体外研究:
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.