EIPA (L593754) 是一种具有口服活性的TRPP3通道抑制剂，IC50为 10.5 μM。EIPA 可通过抑制Na+/H+-exchanger 3(NHE3) 来促进自噬 (autophagy)。EIPA 也抑制巨胞饮作用 (macropinocytosis)。EIPA 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) is an orally activeTRPP3 channelinhibitor with anIC50of 10.5 μM. EIPA also enhancesautophagyby inhibitingNa+/H+-exchanger 3(NHE3). EIPA inhibits macropinocytosis as well. EIPA 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 (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 (300 μM, 6h) enhances autophagy through NHE3 (Na+/H+-exchanger 3) in IEC-18 cells[2].
EIPA (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells[3].
EIPA (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn2+entry in cerebellar granule neurons[4].
EIPA (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression[5].
EIPA (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 (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice[6].
EIPA (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 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(166.80 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液 | 1 mM | 3.3360 mL | 16.6800 mL | 33.3600 mL | | 5 mM | 0.6672 mL | 3.3360 mL | 6.6720 mL | | 10 mM | 0.3336 mL | 1.6680 mL | 3.3360 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.34 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.34 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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