AER-271-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAER-271Cat. No.: HY-115460CAS No.: 634913-39-6分式: CHClFNOP分量: 463.65作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (269.60 mM; Need ultrasonic)Mass Solvent1

2、 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1568 mL 10.7840 mL 21.5680 mL5 mM 0.4314 mL 2.1568 mL 4.3136 mL10 mM 0.2157 mL 1.0784 mL 2.1568 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液

3、中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.49 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.49 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 AER-271AER-270 的膦酸酯前药。AER-271种 aqu

4、aporin-4 (AQP4) 抑制剂，有潜于急性缺性中风的研究 1。IC50 & Target Aquaporin-4 (AQP4) 1体内研究 AER-271 is converted in vivo to AER-270 by endogenous phosphatases. AER-271 blocks acute cerebraledema and improves early outcome in a pediatric model of asphyxial cardiac arrest 1.AER-271 reduces cerebral edema and improves n

5、eurological outcomes in rodent ischemic stroke models.Mice treated with AER-271 (5mg/kg; i.p. injection) show improved outcomes and reduced cerebral edema ina model of ischemic stroke 2.Animal Model: Male mice (C57BL/6J, 8-12week-old, 25-30g) 2Dosage: 5mg/kgAdministration: Treated by i.p. injectionR

6、esult: Had better outcomes with an average neurological score of 0.890.31 compared withcontrol mice receiving vehicle had an average neurological score of 2.500.62.REFERENCES1. Wallisch JS, et al. The aquaporin-4 inhibitor AER-271 blocks acute cerebral edema and improves early outcome in a pediatric

7、 model ofasphyxial cardiac arrest. Pediatr Res. 2019 Mar;85(4):511-517.2. Farr GW, et al. Functionalized Phenylbenzamides Inhibit Aquaporin-4 Reducing Cerebral Edema and Improving Outcome in TwoModels of CNS Injury. Neuroscience. 2019 Apr 15;404:484-498.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use