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Selective glutamate carboxypeptidase II (GCP II) inhibitor (IC50 = 90 nM). Selective for GCP II over NMDA, kainate and AMPA glutamate receptors and MMP-1, -2, -3, -7, -9, ACE and NEP metalloproteases. Antinociceptive in a rat model of neuropathic pain and protects against motor neuron death in familial amyotrophic lateral sclerosis mice. Orally bioavailable.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 206.26. Batch specific molecular weights may vary from batch to batch due to the degree 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||4.85 mL||24.24 mL||48.48 mL|
|5 mM||0.97 mL||4.85 mL||9.7 mL|
|10 mM||0.48 mL||2.42 mL||4.85 mL|
|50 mM||0.1 mL||0.48 mL||0.97 mL|
References are publications that support the biological activity of the product.
Majer et al (2003) Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. J.Med.Chem. 46 1989 PMID: 12723961
Ghadge et al (2003) Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models. Proc.Natl.Acad.Sci.U.S.A. 100 9554 PMID: 12876198
Vornov et al (2013) Pharmacokinetics and pharmacodynamics of the glutamate carboxypeptidase II inhibitor 2-MPPA show prolonged alleviation of neuropathic pain through an indirect mechanism. J.Pharmacol.Exp.Ther. 346 406 PMID: 23776202
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