EIPA-L593754-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEIPACat. No.: HY-101840CAS No.: 1154-25-2Synonyms: L593754; MH 12-43; Ethylisopropylamiloride分式: CHClNO分量: 299.76作靶點: TRP Channel; Sodium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 yearsIn

2、 solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 140 mg/mL (467.04 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.3360 mL 16.6800 mL 33.3600 mL5 mM 0.6672 mL 3.3360 mL 6.6720 mL10 mM 0.3336 mL 1.6680 mL 3.3360 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給

3、藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.33 mg/mL (7.77 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.33 mg/mL (7.77 mM); C

4、lear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 EIPA種 TRPP3 channel 抑制劑，其 IC50 值為 10.5 M。EIPA 還抑制 Na+/H+ 交換 (NHE) 和巨噬細(xì)胞。IC50 & Target IC50: 10.5 M (TRPP3 channel) 1NHE 2Macropinocytosis 3體外研究 In the presence of 500 M amiloride, 100 M EIPA, 10 M benzamil, and 10 M

5、 phenamil, 45Ca2+ uptakedecreases from 799 to 464 (58% remaining), 274 (34%), 295 (37%), and 384 (48%) pmol/oocyte/30min (n=6, P=0.008), respectively. It is found that EIPA, benzamil, and phenamil rapidly and reversibly blockCa2+-activated TRPP3 channel activation at -50 mV, with IC50s of 1438 (n=36

6、), 10.52.2 (n=28), 1.10.3(n=30), and 0.140.04 M (n=25), respectively 1. The number of autophagic vacuoles increasesdramatically in the HAE and HPE groups after EIPA treatment compare with the HAN and HPN groups. EIPAregulates the initiation and maturation of the autophagy associated with amino acids

7、 in IEC-18 cells 2. Inaddition, the uptake of cinnamoylphenazine (CA-PZ) and neutral red (NR) is inhibited by EIPA 3.PROTOCOLCell Assay 2 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

8、for 6 h in DMEM containing 5% FBS and either 0 or 0.3mM EIPA (labelled QNN and QNE, respectively), HBSS containing either 0 or 0.3 mM EIPA (labelled HNNand HNE, respectively), HBSS with 1.0 mM alanine (labelled HAN) or 0.5 mM proline (labelled HPN), HBSSwith 1.0 mM alanine and 0.3 mM EIPA (labelled

9、HAE), and HBSS with 0.5 mM proline and 0.3 mM EIPA(labelled HPE) 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Dai XQ, et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85.2. Shi H, et al. N

10、a+/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.McePdfHeightCaution: Product has not been fully valida