An activator of EAAT2; increases expression of EAAT2 in PA-EAAT2 cells (EC50 = 1.83 μM); selectively increases EAAT2 protein levels over EAAT1 and EAAT3 protein levels and increases glutamate uptake in primary dissociated neuron and astrocyte mixed cultures from 1-3 μM; decreases neuronal loss and degeneration in primary dissociated neuron and astrocyte mixed cultures at 3 μM; increases EAAT2 protein levels and glutamate uptake in mouse forebrain at 40 mg/kg; delays motor function decline and increases lifespan in the SOD1G93A transgenic mouse model of ALS

LDN-0212320 – 10 mg

Brand:
Cayman
CAS:
894002-50-7
Storage:
-20
UN-No:
Non-Hazardous - /

LDN-0212320 is an activator of excitatory amino acid transporter 2 (EAAT2) that increases expression of EAAT2 in PA-EAAT2 cells in a concentration- and time-dependent manner (EC50 = 1.83 μM).{43636} It selectively increases EAAT2 protein levels over EAAT1 and EAAT3 protein levels and increases glutamate uptake in primary dissociated neuron and astrocyte mixed cultures when used at concentrations ranging from 1 to 3 μM. LDN-0212320 (3 μM) decreases neuronal loss and degeneration in primary dissociated neuron and astrocyte mixed cultures. In vivo, LDN-0212320 (40 mg/kg, i.p.) increases EAAT2 protein levels and glutamate uptake in mouse forebrain. It also delays motor function decline and increases lifespan in the SOD1G93A transgenic mouse model of amyotrophic lateral sclerosis (ALS).  

 

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Description

An activator of EAAT2; increases expression of EAAT2 in PA-EAAT2 cells (EC50 = 1.83 μM); selectively increases EAAT2 protein levels over EAAT1 and EAAT3 protein levels and increases glutamate uptake in primary dissociated neuron and astrocyte mixed cultures from 1-3 μM; decreases neuronal loss and degeneration in primary dissociated neuron and astrocyte mixed cultures at 3 μM; increases EAAT2 protein levels and glutamate uptake in mouse forebrain at 40 mg/kg; delays motor function decline and increases lifespan in the SOD1G93A transgenic mouse model of ALS

Formal name: 3-[[(2-methylphenyl)methyl]thio]-6-(2-pyridinyl)-pyridazine

Synonyms:  OSU-0212320

Molecular weight: 293.4

CAS: 894002-50-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Neurodegenerative Disorders

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