WAY-213613 

WAY-213613 is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC₅₀ value of 85 nM. WAY-213613 can be used for the research of central nervous system^[1][2]

WAY-213613 (0-100 μM) has inhibitory activity for human EAAT1, EAAT2 and EAAT3 subtype with IC₅₀ values of 5004 nM, 85 nM and 3787 nM, respectively^[1].
WAY-213613 (3, 30, 300 nM) has the inhibitory effect on synaptosomal L-[³H] glutamate uptake with K_i values of 15 nM, 41 nM and 55 nM in the presence of 3, 30 and 300 nM, respectively^[1].
WAY-213613 (0-100 μM) produces a concentration-dependent block of glutamate-induced currents in EAAT1-, EAAT2- or EAAT3-injected oocytes, with IC₅₀ values of 48, 0.13 and 4.0 μM, respectively^[1].
WAY-213613 (0.5–50 μM) exhibits good selectivity over ionotropic receptors and EAAT2 and potent activity toward blocking NMDA-stimulated responses^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

415.19

C₁₆H₁₃BrF₂N₂O₄

868359-05-1

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]