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2-PMPA

Catalog No. T3440 CAS 173039-10-6

Synonyms: 2-(Phosphonomethyl)pentanedioic acid

2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) (IC50=300 pM).

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2-PMPA, CAS 173039-10-6

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Purity: 98%

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Description	2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) (IC50=300 pM).
Targets&IC50	GCPII:300 pM
In vitro	2-PMPA is a potent and selective inhibitor of GCPII. GCPII is an enzyme that catabolizes the abundant neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to N-acetylaspartate (NAA) and glutamate. 2-PMPA demonstrates robust efficacy in numerous animal models of neurological disease. 2-PMPA is a highly polar compound with multiple negative charges causing significant challenges for analysis in biological matrices[1]. 2-PMPA reduces ketamine-induced decrease of cell viability and increase of LDH levels in the mixed cultures but not in the neuronal cultures[2].
In vivo	Intraperitoneal administration of 100 mg/kg 2-PMPA results in maximum concentration in plasma of 275 μg/mL at 0.25 h. The half-life, area under the curve, apparent clearance, and volume of distribution are 0.64 h, 210 μg×h/mL, 7.93 mL/min/kg, and 0.44 L/kg, respectively[1]. 2-PMPA at 250 mg/kg, in an anesthetized mouse, after an initial rise, produces a rapid decline and a striking attenuation in BOLD signals in gray matter. The signature of 2-PMPA on brain T2* signals in gray matter at both 167 and 250 mg/kg includes a significant initial rise lasting several minutes[3]. 2-PMPA exhibits neuroprotective activity in an animal model of stroke and anti-allodynic activity in CCI model. Administration of 2-PMPA (50 mg/kg) produces a mean peak concentration of 2-PMPA of 29.66±8.1 μM. This concentration is about 100,000 fold more than is needed for inhibition of NAAG peptidase and suggests extremely good penetration to the brain. Administration of 50 mg/kg 2-PMPA (i.p.) produces a continuously increasing extracellular NAAG concentration, which startes directly after application[4].
Cell Research	Neuronal cultures and neuron–glia mixed cultures are treated with ketamine diluted in the culture medium (1, 3, 10, 30, 100, 300, 1000, 2000, 3000 μM) for 24 h to compare neurotoxicity in these two different cell cultures. 2-PMPA is selected to explore the protective effect on ketamine-induced neurotoxicity in these two different cell cultures. Cells are exposed to 2-PMPA (20, 50, 100 μM) half an hour before 10 μM ketamine treatment in neuronal cultures and 2 mM ketamine treatment in neuron–glia mixed cultures for 24 h. Different doses of ketamine chosen in neuronal cultures and neuron–glia mixed cultures are based on the results of cell viability tests[2].

Synonyms	2-(Phosphonomethyl)pentanedioic acid
Molecular Weight	226.12
Formula	C6H11O7P
CAS No.	173039-10-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 28 mg/mL (123.83 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Rais R, et al. Bioanalytical method for evaluating the pharmacokinetics of the GCP-II inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA). J Pharm Biomed Anal. 2014 Jan;88:162-9. 2. Zuo D, et al. Existence of glia mitigated ketamine-induced neurotoxicity in neuron-glia mixed cultures of neonatal rat cortex and the glia-mediated protective effect of 2-PMPA. Neurotoxicology. 2014 Sep;44:218-30. 3. Baslow MH, et al. 2-PMPA, a NAAG peptidase inhibitor, attenuates magnetic resonance BOLD signals in brain of anesthetized mice: evidence of a link between neuron NAAG release and hyperemia. J Mol Neurosci. 2005;26(1):1-15. 4. Nagel J, et al. Effects of NAAG peptidase inhibitor 2-PMPA in model chronic pain-relation to brain concentration. Neuropharmacology. 2006 Dec;51(7-8):1163-71.

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Keywords

2-PMPA 173039-10-6 Proteases/Proteasome Carboxypeptidase inhibit Inhibitor 2PMPA 2-(Phosphonomethyl)pentanedioic acid 2 PMPA inhibitor

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