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2-PMPA

Cat. No. M6154
2-PMPA Structure
Synonym:

2-(Phosphonomethyl)pentanedioic acid

Size Price Availability Quantity
10mg USD 150 In stock
25mg USD 320 In stock
50mg USD 580 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: 2-PMPA is a potent and selective inhibitor of GCPII, an enzyme which 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.

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. 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.

Protocol
Cell Experiment
Cell lines Neuronal cultures
Preparation method 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.
Concentrations 20, 50, 100 μM
Incubation time 24 h
Animal Experiment
Animal models Male Wistar rats
Formulation 50 mM HEPES buffered saline
Dosages 80 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 226.12
Formula C6H11O7P
CAS Number 173039-10-6
Purity >98%
Solubility 28 mg/mL in water
Storage at -20°C
References

Bioanalytical method for evaluating the pharmacokinetics of the GCP-II inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA).
Rais R, et al. J Pharm Biomed Anal. 2014 Jan;88:162-9. PMID: 24055700.

NAAG peptidase inhibitors block cognitive deficit induced by MK-801 and motor activation induced by d-amphetamine in animal models of schizophrenia.
Olszewski RT, et al. Transl Psychiatry. 2012 Jul 31;2:e145. PMID: 22850437.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: 2-PMPA, 2-(Phosphonomethyl)pentanedioic acid supplier, inhibitors

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