1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZL006Cat. No.: HY-100456CAS No.: 1181226-02-7分式: CHClNO分量: 328.15作靶點: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 29 mg/mL

2、(88.37 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.0474 mL 15.2369 mL 30.4739 mL5 mM 0.6095 mL 3.0474 mL 6.0948 mL10 mM 0.3047 mL 1.5237 mL 3.0474 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。BIOLOGICAL ACTIVITY物活性 ZL006nNOS/PSD-95 相互作的抑制劑，可抑制 nMD

3、A receptor 誘導(dǎo)的氧化氮的合成。體外研究ZL006 presents little cytotoxicity, and a growth inhibition of BCECs is not found at low concentration of 0.001,0.01, 0.1, 1 and 10 g/mL. The cytotoxicity of T7-P-LPs/ZL006 is significantly enhanced at the concentrationof 10 g/mL. Cellular uptake of ZL006 loads P-LPs and T7-

4、P-LPs after incubation for 0.5 h at theconcentrations range from 100 g/mL to 600 g/mL in BCECs 1. ZL006 does not inhibit the nNOS-1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEPDZ/PSD-95-PDZ interaction, or perturb the nNOS -finger 2.體內(nèi)研究 Compared with P-LPs/ZL006 and free ZL006, T7-P-LPs/ZL006 e

5、xhibits a significant increase of drugaccumulation in the brain tissue due to its better brain targeting delivery. Compared with free ZL006, P-LPs/ZL006 and T7-P-LPs/ZL006 exhibit a significant decrease of drug accumulation in the liver and kidney1.PROTOCOLCell Assay 1 BCECs are seeded in 96-well pl

6、ates in 200 L of DMEM medium to obtain a concentration of 2000 cells perwell, and incubated for 24 h. The medium in each well is then incubated for 72 h with 200 L mediumcontaining blank vehicle, P-LPs/ZL006, T7-P-LPs/ZL006 and ZL006 (free drug dissolved in DMSO) with aseries of concentrations rangi

7、ng from 0.001 to 100 g/mL. The MTT absorbance at 570 nm of each well ismeasured by a microplate reader.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal ICR mice weighting 20 2 g are divided into three groups at random (n=12). Free ZL006, P-LPs/ZL0

8、06 andAdministration 1 T7-P-LPs/ZL006 (all containing ZL006 4 mg/kg) are administered to each group through intravenous route,respectively. At designated time intervals (0.5, 1 and 2 h), the mice are executed and the major organssamples including brain, heart, liver, spleen, lung and kidney are coll

9、ected. Before pretreatment, thesetissues are rinsed with cold saline solution to remove the blood and then blotted with paper towel. Proteinprecipitation of the samples is performed before analysis. Then the samples are injected into the LC-MS/MSsystems for analysis. The LC-MS/MS system consists of

10、an Agilent Series 1200 HPLC system and a 6410Triple Quad LC/MS mass spectrometer. The data is collected and processed using the Agilent MassHunterWorkstation Software.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Wang Z, et al. Enhanced a

11、nti-ischemic stroke of ZL006 by T7-conjugated PEGylated liposomes drug delivery system. Sci Rep. 2015 Jul29;5:12651.2. Bach A, et al. Biochemical investigations of the mechanism of action of small molecules ZL006 and IC87201 as potential inhibitors of thenNOS-PDZ/PSD-95-PDZ interactions. Sci Rep. 2015 Jul 16;5:12157.McePdfHeightCaution: Product has not