PMPA(NAALADaseinhibitor)
PMPA(NAALADaseinhibitor) Basic information
- Product Name:
- PMPA(NAALADaseinhibitor)
- Synonyms:
-
- PMPA(NAALADaseinhibitor)
- 2-(Phosphonomethyl)pentane-1,5-dioicacid
- 2-PMPA
- CS-2454
- 2-PMPA(NAALADaseinhibitor)
- NAALADASEINHIBITOR
- Pentanedioic acid, 2-(phosphonomethyl)-
- 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID (PMPA)
- CAS:
- 173039-10-6
- MF:
- C6H11O7P
- MW:
- 226.12
- Mol File:
- 173039-10-6.mol
PMPA(NAALADaseinhibitor) Chemical Properties
- Boiling point:
- 538.8±60.0 °C(Predicted)
- Density
- 1.658±0.06 g/cm3(Predicted)
- storage temp.
- room temp
- solubility
- Soluble to 100 mM in sterile
- form
- powder
- pka
- 2.06±0.10(Predicted)
- color
- white to beige
- Water Solubility
- Soluble to 100 mM in water
PMPA(NAALADaseinhibitor) Usage And Synthesis
Uses
2-(Phosphonomethyl)pentanedioic Acid is a selective glutamate carboxypeptidase 2 (GCP-II) inhibitor, the enzyme which catabolizes the abundant neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to N-acetylaspartate (NAA) and glutamate. A posiible target in the treatment of multiple sclerosis and Schizophrenia.
Biological Activity
Highly potent and selective inhibitor of? glutamate carboxypeptidase 2 (GCP II/N-acetylated α -linked dipeptidase/NAALADase) with a K i value of 275 pM. Neuroprotective; protects against glutamate-mediated motor neuron degeneration and reduces volume of injury following middle cerebral artery occlusion (MCAO).
Biochem/physiol Actions
2-PMPA is a potent and selective inhibitor of Glutamate carboxypeptidase II (GCPII).
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 has neuroprotective activity in an animal model of stroke and anti-allodynic activity in CCI model. Administration of 2-PMPA (50mg/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 indicates very 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].
storage
Desiccate at RT
PMPA(NAALADaseinhibitor)Supplier
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