2-MPPA

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Cat.No. 5033 - 2-MPPA | C8H14O4S | CAS No. 254737-29-6
Description: Selective glutamate carboxypeptidase II (GCP II) inhibitor; orally bioavailable
Chemical Name: 2-(3-Mercaptopropyl)pentanedioic acid
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Citations
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Literature

Biological Activity

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.

Technical Data

M. Wt 206.26
Formula C8H14O4S
Storage Store at -20°C
CAS Number 254737-29-6
PubChem ID 10198171
InChI Key FNLNSQHJKVQCBP-UHFFFAOYSA-N
Smiles SCCCC(C(O)=O)CCC(O)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.63 100
water 20.63 100

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 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 4.85 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

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References

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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Citations for 2-MPPA

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