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编 号:F128722
分子式:C11H19Cl2N7O
分子量:336.22
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10mM*1mL in DMSO
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5mg
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10mg
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生物活性:
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.

体内研究:
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.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 hydrochloride (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 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 Zn2+ 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.
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