EIPA

SKU: orb1219965

Description

EIPA (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.It is found that EIPA, benzamil, and phenamil rapidly and reversibly block Ca2+-activated TRPP3 channel activation at -50 mV, with IC50s of 143, 10.5, 1.1, and 0.14 μM, respectively. The number of autophagic vacuoles increases dramatically in the HAE and HPE groups after EIPA treatment compares with the HAN and HPN groups. EIPA regulates the initiation and maturation of the autophagy associated with amino acids in IEC-18 cells. In addition, the uptake of cinnamoylphenazine (CA-PZ) and neutral red (NR) is inhibited by EIPA.(In Vitro):EIPA (100 μM, 30 min) suppresses TRPP3-mediated Ca2+ uptake in X. laevis oocytes. EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na+ current (IC50: 19.5 μM). EIPA (300 μM, 6h) enhances autophagy through NHE3 (Na+/H+-exchanger 3) in IEC-18 cells. EIPA (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells. EIPA (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn2+ entry in cerebellar granule neurons. EIPA (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression. EIPA (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein.(In Vivo):EIPA (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice.EIPA (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model.

Key Properties

• CAS Number: 1154-25-2
• MW: 299.76
• Purity: >98% (HPLC)
• Formula: C₁₁H₁₈ClN₇O
• SMILES: CCN(C(C)C)c1nc(N)c(nc1Cl)C(=O)NC(N)=N
• Target: TRP/TRPV Channel
• Solubility: DMSO:135 mg/mL (450.36 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  EIPA (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice. EIPA (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model. Animal model: Male ddY strain mice. 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. 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.
• In Vitro:
  EIPA (100 μM, 30 min) suppresses TRPP3-mediated Ca2+ uptake in X. laevis oocytes. EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na+ current (IC50: 19.5 μM). EIPA (300 μM, 6h) enhances autophagy through NHE3 (Na+/H+-exchanger 3) in IEC-18 cells. EIPA (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells. EIPA (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn2+ entry in cerebellar granule neurons. EIPA (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression. EIPA (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein. Cell Proliferation Assay. 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. Cell line: IEC-18 cells. Concentration: 300 μM. Incubation time: 6 h. Result: Increased total LC3-II protein levels and P62 flux.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

L593754,MH 12-43

Quick Database Links

Gene Symbol

TRP/TRPV Channel