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5-(N-ethyl-N-isopropyl)amiloride
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
5-(N-ethyl-N-isopropyl)amiloride (EIPA) is a potent small-molecule analog of the diuretic amiloride. It acts primarily as an inhibitor of the sodium-hydrogen exchanger (NHE) family, with high affinity for isoforms such as NHE1, NHE5, and NHE8. EIPA is widely recognized in cell biology as a gold-standard pharmacological inhibitor of macropinocytosis, a clathrin-independent endocytic process. By inhibiting NHEs, EIPA prevents the sub-membranous acidification required for actin remodeling and macropinosome formation. Beyond its role in pH regulation and endocytosis, EIPA has been shown to inhibit the Na+/Ca2+ exchanger (NCX1) and mitochondrial respiratory complex I. In preclinical research, it is investigated for its potential to sensitize cancer cells to radiotherapy, modulate alternative splicing of the SMN2 gene in spinal muscular atrophy models, and block the entry of various viruses, including Chikungunya and Human Cytomegalovirus.
- Other names
- 5-(N-Ethyl-N-isopropyl)amilorideEthylisopropylamiloride
02
Targets
ASIC (ASIC family)PKD2L1 (Polycystin-2-like 1 ion channel)
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