A potent inhibitor of GCP II/NAALADase (Ki = 98 pM for release of glutamate from the NAALADase peptide substrate NAAG); selective for GCP II/NAALADase over a panel of 100 receptors

2-(Phosphonomethyl)-pentanedioic Acid – 1 mg

Brand:
Cayman
CAS:
173039-10-6
Storage:
-20
UN-No:
Non-Hazardous - /

2-(Phosphonomethyl)-pentanedioic acid (2-PMPA) is a potent inhibitor of glutamate carboxypeptidase II (GCP II), also known as N-acetylated α-linked dipeptidase (NAALADase), with a Ki value of 98 pM for release of glutamate from the NAALADase peptide substrate N-acetylasparatylglutamate (NAAG).{38879} It is selective for GCP II/NAALADase over a panel of 100 receptors, transporters, ion channels, and enzymes at a concentration of 10 μM.{7392} 2-PMPA is neuroprotective against hypoxia (EC50 = 8.4 μM), but not veratridine-induced injury, in neuron-enriched primary cultures from rat embryo cerebellum.{38880} In vivo, 2-PMPA reduces neuronal cell death induced by middle cerebral artery occlusion via increases in NAAG expression and reduction of glutamate in rats.{7392} 2-PMPA (100 mg/kg) blocks the conditioned place preference response to cocaine, but not food, in male rats.{38881} It reduces the number of flinches induced by formalin injection into the footpad of mice when administered at a dose of 10 μg per animal, an effect that is reversed by the group II metabotropic glutamate receptor antagonist LY341495.{38878} 2-PMPA also decreases severity and delays onset of experimental autoimmune encephalomyelitis (EAE) in mice.{38882}  

 

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Description

A potent inhibitor of GCP II/NAALADase (Ki = 98 pM for release of glutamate from the NAALADase peptide substrate NAAG); selective for GCP II/NAALADase over a panel of 100 receptors, transporters, ion channels, and enzymes at a concentration of 10 μM; neuroprotective against hypoxia (EC50 = 8.4 μM) in neuron-enriched primary cultures from rat embryo cerebellum; reduces neuronal cell death induced by middle cerebral artery occlusion in rats; blocks the conditioned place preference response to cocaine in male rats (100 mg/kg); reduces the number of flinches induced by formalin injection into the footpad of mice (10 μg per animal); decreases severity and delays onset of EAE in mice,

Formal name: 2-(phosphonomethyl)-pentanedioic acid

Synonyms:  2-PMPA

Molecular weight: 226.1

CAS: 173039-10-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Neuroprotection||Research Area|Neuroscience|Pain Research

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