| 产品描述： | EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma |
| 靶点： |
COX-2;SodiumChannel; TRP/TRPVChannel |
| 体内研究： |
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 |
| 参考文献： |
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. 4. E V Stelmashook, et al. Acidosis and 5-(N-ethyl-N-isopropyl)amiloride (EIPA) Attenuate Zinc/Kainate Toxicity in Cultured Cerebellar Granule Neurons. Biochemistry (Mosc). 2015 Aug;80(8):1065-72. 5. Shigekuni Hosogi, et al. An inhibitor of Na(+)/H(+) exchanger (NHE), ethyl-isopropyl amiloride (EIPA), diminishes proliferation of MKN28 human gastric cancer cells by decreasing the cytosolic Cl(-) concentration via DIDS-sensitive pathways. Cell Physiol Biochem. 2012;30(5):1241-53. 6. Junji Yamashita, et al. Role of Na+/H+ exchanger in the pathogenesis of ischemic acute renal failure in mice. J Cardiovasc Pharmacol. 2007 Mar;49(3):154-60. 7. Fumitaka Kamachi, et al. Inhibition of lipopolysaccharide-induced prostaglandin E2 production and inflammation by the Na+/H+ exchanger inhibitors. J Pharmacol Exp Ther. 2007 Apr;321(1):345-52. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
2-8℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.336 ml |
16.68 ml |
33.36 ml |
| 5 mM |
0.667 ml |
3.336 ml |
6.672 ml |
| 10 mM |
0.334 ml |
1.668 ml |
3.336 ml |
| 50 mM |
0.067 ml |
0.334 ml |
0.667 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京