| MDL | - |
|---|---|
| Molecular Weight | 336.22 |
| Molecular Formula | C11H19Cl2N7O |
| SMILES | O=C(C1=NC(Cl)=C(N(CC)C(C)C)N=C1N)NC(N)=N.Cl |
EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC 50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na + /H + -exchanger 3 ( NHE3 ). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer , colon carcinoma, pancreatic carcinoma [1] [2] [3] [5] .
|
COX-2 |
EIPA hydrochloride (100 μM, 30 min) suppresses TRPP3-mediated Ca
2+
uptake in
X. laevis oocytes
[1]
.
EIPA hydrochloride (10-100 μM) reversibly inhibits the basal Na
+
current (IC
50
: 19.5 μM)
[1]
.
EIPA hydrochloride (300 μM, 6h) enhances autophagy through NHE3 (Na
+
/H
+
-exchanger 3) in IEC-18 cells
[2]
.
EIPA hydrochloride (20 μM, 2 h) blocks macropinocytosis-mediated uptake of CA-PZ massively entry in HT-29 cells and MIA PaCa-2 cells
[3]
.
EIPA hydrochloride (30 μM, 3h) attenuates Zinc/Kainate toxicity by decreasing Zn
2+
entry in cerebellar granule neurons
[4]
.
EIPA hydrochloride (5-100 μM, 48h) suppresses proliferation of MKN28 cells through up-regulation of p21 expression
[5]
.
EIPA hydrochloride (3 μM, 6 h) inhibits the LPS-induced increase in the level of COX-2 protein
[7]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
EIPA hydrochloride (Intravenous injection, 1 mg/kg) dose-dependently attenuates the I/R (Ischemia/reperfusion)-induced renal dysfunction in ddY strain mice
[6]
.
EIPA hydrochloride (oral administration, 10 mg/kg) inhibits LPS-induced inflammation in air pouch-type LPS-induced inflammation model
[7]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
DMSO : 130 mg/mL ( 386.65 mM ; Need ultrasonic)
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9742 mL | 14.8712 mL | 29.7424 mL |
| 5 mM | 0.5948 mL | 2.9742 mL | 5.9485 mL |
| 10 mM | 0.2974 mL | 1.4871 mL | 2.9742 mL |