EIPA

SKU: orb1296167

Description

EIPA (L593754) is a dual inhibitor of TRPP3 channels (IC50=10.5 μM) and Na+/H+ exchangers (NHE). It is a research tool used to study autophagy, cell volume regulation, and processes relevant to cancer and inflammatory disease models in both cellular and animal studies.

Research Area

Cell Biology, Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1154-25-2
• MW: 299.76
• Purity: 99.98% (May vary between batches)
• Formula: C₁₁H₁₈ClN₇O
• SMILES: CCN(C(C)C)c1nc(N)c(nc1Cl)C(=O)NC(N)=N
• Target: Prostaglandin Receptor,TRP/TRPV Channel,Sodium Channel,COX,Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (13.34 mM);DMSO:135 mg/mL (450.36 mM)

Bioactivity

• Target IC50:
  TRPP3 channel:10.5 μM
• In Vivo:
  METHODS: To assay in vivo activity, EIPA (10 mg/kg) was injected intraperitoneally into BALB/c mice bearing 4T1 xenografts, and 70 kD FITC-Ficoll was injected into the tumors 1 h later. The mice were necropsied 1 h after Ficoll injection, and the tumors were excised and frozen in OCT. RESULTS: EIPA-sensitive 70 kD FITC-Ficoll uptake was observed in in situ homozygous 4T1 tumors of BALB/c mice, suggesting that AMPK activation or other signals are sufficient to trigger the formation of large fusions in vivo.
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• In Vitro:
  METHODS: Ten cells were pretreated with EIPA (50 µM) for 1.5 h. Dextran index was measured by Dextran uptake assay. RESULTS: Immortalized but untransformed hTERT-HME1 mammary epithelial cells and MCF10A cells did not exhibit megacellular drinking in complete medium, but stimulated dextran uptake by nutrient deprivation. Although PIK3CB was found to be required for growth factor-stimulated macrocytosis, oncogenic mutations in PIK3CA were sufficient to induce constitutive macrocytosis in mouse embryonic fibroblast MEFs and untransformed MCF10A cells. METHODS: MKN28 cells were treated with EIPA (5-100 µM) for 48 h. Cell proliferation was detected by cell count. RESULTS: Cell exposure to EIPA inhibited the proliferation of MKN28 cells in a dose- and time-dependent manner.
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• Cell Research:
  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 (labeled QNN and QNE, respectively), HBSS containing either 0 or 0.3 mM EIPA (labeled HNN and HNE, respectively), HBSS with 1.0 mM alanine (labeled HAN) or 0.5 mM proline (labeled HPN), HBSS with 1.0 mM alanine and 0.3 mM EIPA (labeled HAE), and HBSS with 0.5 mM proline and 0.3 mM EIPA (labeled HPE) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Sodium Channel, Sodium-hydrogen Exchanger, Sodium/hydrogen Exchanger, SodiumChannel, zinc, Prostaglandin Receptor, renal failure, Transient receptor potential channels, TRP Channel, TRPVChannel, TRPV Channel, TRPP3 channel, TRPChannel, MH 12-43, pancreatic carcinoma, NHE3, Na+/H+ Exchanger (NHE), Na+/H+-exchanger (NHE), MKN28, neuron, kainite, inhibit, L 593754, Inhibitor, gastric cancer, IEC-18, IECs, IBDs, L593754, L-593754, EIPA, ddY strain mice, Cyclooxygenase, COX, colon carcinoma, Autophagy, calcium, Cation channel

Compound Identifiers

PubChem CID

1795