EIPA (L593754) is a TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA also inhibits Na⁺/H⁺-exchanger (NHE) and macropinocytosis^[1][2][3].

IC50: 10.5 μM (TRPP3 channel)^[1]
NHE^[2]
Macropinocytosis^[3]

In the presence of 100 μM EIPA, 10 μM benzamil, and 10 μM phenamil, ⁴⁵Ca²⁺ uptake decreases from 79±9 to 46±4 (58% remaining), 27±4 (34%), 29±5 (37%), and 38±4 (48%) pmol/oocyte/30 min (n=6, P=0.008), respectively. It is found that EIPA, benzamil, and phenamil rapidly and reversibly block Ca²⁺-activated TRPP3 channel activation at -50 mV, with IC₅₀s of 143±8 (n=36), 10.5±2.2 (n=28), 1.1±0.3 (n=30), and 0.14±0.04 μM (n=25), respectively^[1]. The number of autophagic vacuoles increases dramatically in the HAE and HPE groups after EIPA treatment compare with the HAN and HPN groups. EIPA regulates the initiation and maturation of the autophagy associated with amino acids in IEC-18 cells^[2]. In addition, the uptake of cinnamoylphenazine (CA-PZ) and neutral red (NR) is inhibited by EIPA^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

299.76

C₁₁H₁₈ClN₇O

1154-25-2

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 140 mg/mL (467.04 mM; Need ultrasonic)

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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: ≥ 2.33 mg/mL (7.77 mM); Clear solution

  此方案可获得 ≥ 2.33 mg/mL (7.77 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 23.3 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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.33 mg/mL (7.77 mM); Clear solution

  此方案可获得 ≥ 2.33 mg/mL (7.77 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 23.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [1]. Dai XQ, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85.

  [2]. Shi H, et al. Na+/H+ Exchanger Regulates Amino Acid-Mediated Autophagy in Intestinal Epithelial Cells. Cell Physiol Biochem. 2017;42(6):2418-2429.

  [3]. Zhu BY, et al. A new HDAC inhibitor cinnamoylphenazine shows antitumor activity in association with intensive macropinocytosis.

The effect of EIPA alone (without alanine or proline) is also examined in both control (DMEM cultured cells) and amino acid-starved cells. The cells are incubated for 6 h in DMEM containing 5% FBS and either 0 or 0.3 mM EIPA (labelled QNN and QNE, respectively), HBSS containing either 0 or 0.3 mM EIPA (labelled HNN and HNE, respectively), HBSS with 1.0 mM alanine (labelled HAN) or 0.5 mM proline (labelled HPN), HBSS with 1.0 mM alanine and 0.3 mM EIPA (labelled HAE), and HBSS with 0.5 mM proline and 0.3 mM EIPA (labelled HPE)^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Dai XQ, et al. Inhibition of TRPP3 channel by MK-870 and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85.

  [2]. Shi H, et al. Na+/H+ Exchanger Regulates Amino Acid-Mediated Autophagy in Intestinal Epithelial Cells. Cell Physiol Biochem. 2017;42(6):2418-2429.

  [3]. Zhu BY, et al. A new HDAC inhibitor cinnamoylphenazine shows antitumor activity in association with intensive macropinocytosis.