PMPA (NAALADase inhibitor)
Highly potent and selective inhibitor of glutamate carboxypeptidase 2 (GCP II/N-acetylated α-linked dipeptidase/NAALADase) with a Ki value of 275 pM. Neuroprotective; protects against glutamate-mediated motor neuron degeneration and reduces volume of injury following middle cerebral artery occlusion (MCAO).
Sold with the permission of AstraZeneca Ltd.
|Storage||Desiccate at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 226.12. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.42 mL||22.11 mL||44.22 mL|
|5 mM||0.88 mL||4.42 mL||8.84 mL|
|10 mM||0.44 mL||2.21 mL||4.42 mL|
|50 mM||0.09 mL||0.44 mL||0.88 mL|
References are publications that support the biological activity of the product.
Jackson et al (1996) Design, synthesis, and biological activity of a potent inhibitor of the neuropeptidase N-acetylated α-linked acidic dipeptidase. J.Med.Chem. 39 619 PMID: 8558536
Slusher et al (1999) Selective inhibition of NAALADase, which converts NAAG to glutamate, reduces ischemic brain injury. Nat.Med. 5 1396 PMID: 10581082
Thomas et al (2003) NAALADase inhibition protects motor neurons against chronic glutamate toxicity. Eur.J.Pharmacol. 471 177 PMID: 12826236
Rahn et al (2012) Inhibition of glutamate carboxypeptidase II (GCPII) activity as a treatment for cognitive impairment in multiple sclerosis. Proc.Natl.Acad.Sci.U S A (Epub ahead of print] PMID: 23169655
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Keywords: PMPA (NAALADase inhibitor), PMPA (NAALADase inhibitor) supplier, potent, selective, NAALADase, GCP, II, inhibitors, inhibits, Carboxypeptidase, NAAG, Peptidase, Proteinases, Proteases, AstraZeneca, Miscellaneous, Glutamate, 1380, Tocris Bioscience
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