2-MPPA

Cat. No. 5033 Submit a Review Datasheet / COA / SDS

Description: Selective glutamate carboxypeptidase II (GCP II) inhibitor; orally bioavailable

Chemical Name: 2-(3-Mercaptopropyl)pentanedioic acid

Datasheet

Citations

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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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

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

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Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

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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