EIPA

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EIPA (L593754, MH 12-43) 是一种 TRPP3 通道抑制剂 (IC50: 10.5 μM)。它还抑制Na+/H+-交换器(NHE)和巨胞饮作用。发现EIPA、benzamil和phenamil在-50 mV下快速可逆地阻断Ca2+激活的TRPP3通道激活，IC50分别为143、10.5、1.1和0.14分别为μM。

EIPA (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.It is found that EIPA, benzamil, and phenamil rapidly and reversibly block Ca2+-activated TRPP3 channel activation at -50 mV, with IC50s of 143, 10.5, 1.1, and 0.14 μM, respectively. The number of autophagic vacuoles increases dramatically in the HAE and HPE groups after EIPA treatment compares with the HAN and HPN groups. EIPA regulates the initiation and maturation of the autophagy associated with amino acids in IEC-18 cells. In addition, the uptake of cinnamoylphenazine (CA-PZ) and neutral red (NR) is inhibited by EIPA.(In Vitro):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.(In Vivo):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.

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. Cell Proliferation Assay Cell Line:MKN28 cells Concentration:5, 10, 25, 50, and 100 μM Incubation Time:48 h Result:Inhibited cell proliferation in a dose- and time-dependent manner.Western Blot Analysis Cell Line:IEC-18 cells Concentration:300 μM Incubation Time:6 h Result:Increased total LC3-II protein levels and P62 flux.

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 modelDosage: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.

L593754,MH 12-43

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPP3 channel| Na+/H+-exchanger (NHE)

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1154-25-2

299.76

C11H18ClN7O

>98% (HPLC)

DMSO:135 mg/mL (450.36 mM; Need ultrasonic)

CCN(C(C)C)c1nc(N)c(nc1Cl)C(=O)NC(N)=N

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(-20℃)

With Ice Pack

≥ 2 years