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2-PMPA tetrasodium

Cat. No. M6154
2-PMPA tetrasodium Structure
Synonym:

PMPA tetrasodium salt; 2-(Phosphonomethyl)pentanedioic acid

Size Price Availability Quantity
10mg USD 150  USD150 In stock
25mg USD 320  USD320 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

In vitro: 2-PMPA (PMPA tetrasodium salt) 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.

CAS#: 173039-10-6(free base)

Product Citations
Customer Product Validations & Biological Datas
Source Front Cell Dev Biol (2021 Mar). Figure 3. 2-PMPA (Abmole Bioscience, USA)
Method Cell Culture
Cell Lines HUVECs, U87 and U251 cell lines
Concentrations 100 µM
Incubation Time 24 h
Results Meanwhile, the treatment of PSMA inhibitor 2-PMPA could effectively eliminate PSMA expression in all groups
Protocol (for reference only)
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.
Chemical Information
Molecular Weight 314.05
Formula C6H7Na4O7P
CAS Number 373645-42-2
Solubility (25°C) Water ≥ 10 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Rais R, et al. J Pharm Biomed Anal. Bioanalytical method for evaluating the pharmacokinetics of the GCP-II inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA).

[2] Olszewski RT, et al. Transl Psychiatry. NAAG peptidase inhibitors block cognitive deficit induced by MK-801 and motor activation induced by d-amphetamine in animal models of schizophrenia.

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Keywords: 2-PMPA tetrasodium, PMPA tetrasodium salt; 2-(Phosphonomethyl)pentanedioic acid supplier, inhibitors, activators


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