c-Met/HGFR Activator

Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (K_d=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease.

Terevalefim (ANG-3777), an hepatocyte growth factor (HGF) mimetic, selectively activates the c-Met receptor.

MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 reduces NF-κB p65 expression. MY10 activates tyrosine phosphorylation of c-Met. MY10 prevents the alcohol-induced downregulation of Ptprz1 and Alk expression. MY10 attenuates binge-like ethanol consumption and ethanol reward. MY10 can be used in the study of neurological and vascular diseases.

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.