WAY 213613 是一种有效的选择性人 EAAT2 抑制剂。
Cas No. | 868359-05-1 |
别名 | N-[4-(2-溴-4,5-二氟苯氧基)苯基]-L-天冬酰胺 |
化学名 | (S)-2-amino-4-((4-(2-bromo-4,5-difluorophenoxy)phenyl)amino)-4-oxobutanoic acid |
Canonical SMILES | BrC(C(OC1=CC=C(C=C1)NC(C[C@@H](C(O)=O)N)=O)=C2)=CC(F)=C2F |
分子式 | C16H13BrF2N2O4 |
分子量 | 415.19 |
溶解度 | <41.51mg/ml in DMSO;<41.51mg/ml in 1eq. NaOH |
储存条件 | Desiccate at RT |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | WAY-213613 is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2. It displays 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC50s are 5 and 3.8 μM, respectively). WAY-213613 shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function[1][2]. References: [1]. Dunlop J, et al. Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2. Mol Pharmacol. 2005 Oct;68(4):974-82. Epub 2005 Jul 13. [2]. Simmons DA, et al. A small molecule p75NTR ligand, LM11A-31, reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression. PLoS One. 2014 Aug 25;9(8):e102136. |