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Home   »   Product Pathways  »  Carboxypeptidase  »  2-PMPA

Products are for research use only. Not for human use. We do not sell to patients.


CS-6202 2-PMPA


(2-(Phosphonomethyl)pentanedioic acid)
Structure Price and Availability of    2-PMPA
United States
Size Price Stock
5mg $75 In-stock Inquiry
10mg $130 In-stock
25mg $290 In-stock
50mg $520 In-stock
100mg $940 In-stock
200 mg Get quote
500 mg Get quote
 Distributor In Japan:  フナコシ株式会社 www.funakoshi.co.jp    電話番号:81-3-5684-1620   
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  • Data Sheet
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2-PMPA  M.Wt:  226.12
2-PMPA  Formula: C6H11O7P
2-PMPA  Solubility: 10 mM in DMSO
2-PMPA  Purity: >98%
2-PMPA  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 173039-10-6

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2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM. IC50&Target: 300 pM (GCPII)[1] InVitro: 2-PMPA 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[1]. 2-PMPA reduces ketamine-induced decrease of cell viability and increase of LDH levels in the mixed cultures but not in the neuronal cultures[2]. InVivo: 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[1]. 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[3]. 2-PMPA has neuroprotective activity in an animal model of stroke and anti-allodynic activity in CCI model. Administration of 2-PMPA (50mg/kg) produces a mean peak concentration of 2-PMPA of 29.66±8.1 μM. This concentration is about 100,000 fold more than is needed for inhibition of NAAG peptidase, and indicates very good penetration to the brain. Administration of 50 mg/kg 2-PMPA (i.p.) produces a continuously increasing extracellular NAAG concentration, which startes directly after application[4].

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