EIPA (L593754) hydrochloride 是一种具有口服活性的TRPP3通道抑制剂，IC50为 10.5 μM。EIPA hydrochloride 可通过抑制Na+/H+-exchanger 3(NHE3) 来促进自噬 (autophagy)。EIPA hydrochloride 也抑制巨胞饮作用 (macropinocytosis)。EIPA hydrochloride 可用于炎症和癌症的研究，如胃癌、结肠癌、胰腺癌。
| 生物活性 | EIPA (L593754) hydrochloride is an orally activeTRPP3 channelinhibitor with anIC50of 10.5 μM. EIPA hydrochloride also enhancesautophagyby inhibitingNa+/H+-exchanger 3(NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastriccancer, colon carcinoma, pancreatic carcinoma[1][2][3][5]. |
| IC50& Target[7] | |
体外研究
(In Vitro) | EIPA hydrochloride (100 μM, 30 min) suppresses TRPP3-mediated Ca2+uptake inX. laevis oocytes[1].
EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na+current (IC50: 19.5 μM)[1].
EIPA hydrochloride (300 μM, 6h) enhances autophagy through NHE3 (Na+/H+-exchanger 3) in IEC-18 cells[2].
EIPA hydrochloride (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells[3].
EIPA hydrochloride (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn2+entry in cerebellar granule neurons[4].
EIPA hydrochloride (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression[5].
EIPA hydrochloride (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein[7].
Cell Proliferation Assay[5] | 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[2] | Cell Line: | IEC-18 cells | | Concentration: | 300 μM | | Incubation Time: | 6 h | | Result: | Increased total LC3-II protein levels and P62 flux.
Increased ATG5, 7, 12 and P62 expression. |
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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[6].
EIPA hydrochloride (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model[7].
| Animal Model: | Male ddY strain mice[6] | | 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[7] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 130 mg/mL(386.65 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.9742 mL | 14.8712 mL | 29.7424 mL | | 5 mM | 0.5948 mL | 2.9742 mL | 5.9485 mL | | 10 mM | 0.2974 mL | 1.4871 mL | 2.9742 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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