EAAT2 Activator

LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC^[1]

Brelgometon (ATH-1105) is an orally active HGF/MET positive modulator. Brelgometon activates downstream ERK and AKT cascades. Brelgometon reduces pro-inflammatory cytokine levels and extranuclear TDP-43 aggregation; it also upregulates EAAT2 expression and improves mitochondrial function. Brelgometon protects neurons from excitotoxicity, inflammation, oxidative stress and mitochondrial dysfunction; it also maintains neurite length, neuromuscular junction integrity and sciatic nerve function. Brelgometon alleviates motor function deterioration, maintains body weight and prolongs survival in ALS transgenic mice. Brelgometon is applicable to research related to amyotrophic lateral sclerosis.

HCM-01 is an Excitatory amino acid transporter 2 (EAAT2) activator with oral effectiveness and blood-brain barrier penetration.HCM-01 binds to the allosteric site of EAAT2, increases EAAT2 expression in astrocytes, enhances glutamate-handling capacity, and modulates glutamate homeostasis.HCM-01 acts as an antioxidant, improves oxidative/antioxidative balance and increases total antioxidant capacity. HCM-01 can be used for the research of Alzheimer's disease.

EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently.