WAY-213613_product_DataBase

Bioactivity

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]

Target

IC50: 5004 nM (EAAT1); 85 nM (EAAT2); 3787 nM (EAAT3)

Invitro

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 Ki 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-dependentblock of glutamate-induced currents in EAAT1-, EAAT2- orEAAT3-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].

Name

WAY-213613

CAS

868359-05-1

Formula

C16H13BrF2N2O4

Molar Mass

415.19

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

WAY-213613

CAS: 868359-05-1 F: C16H13BrF2N2O4 W: 415.19