2. Metabolic Enzyme/Protease
  3. Carboxypeptidase
  4. 2-PMPA

2-PMPA  (Synonyms: 2-(Phosphonomethyl)pentanedioic acid)

Cat. No.: HY-100788 Purity: ≥98.0%
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2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM.

For research use only. We do not sell to patients.

2-PMPA Chemical Structure

2-PMPA Chemical Structure

CAS No. : 173039-10-6

Size Price Stock Quantity
Oil + Solvent
10 mM * 1 mL in Water
ready for reconstitution
 USD 85 In-stock
Solution
10 mM * 1 mL in Water USD 85 In-stock
Oil
5 mg USD 77 In-stock
10 mg USD 121 In-stock
25 mg USD 242 In-stock
50 mg USD 352 In-stock
100 mg USD 572 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

2-PMPA Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM.

IC50 & Target

IC50: 300 pM (GCPII)[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

2-PMPA Related Antibodies
In Vivo

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

226.12

Formula

C6H11O7P
CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

O=C(O)C(CP(O)(O)=O)CCC(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : ≥ 28 mg/mL (123.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4224 mL 22.1122 mL 44.2243 mL
5 mM 0.8845 mL 4.4224 mL 8.8449 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (442.24 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
Cell Assay
[2]

Neuronal cultures and neuron–glia mixed cultures are treated with ketamine diluted in the culture medium (1, 3, 10, 30, 100, 300, 1000, 2000, 3000 μM) for 24 h to compare neurotoxicity in these two different cell cultures. 2-PMPA is selected to explore the protective effect on ketamine-induced neurotoxicity in these two different cell cultures. Cells are exposed to 2-PMPA (20, 50, 100 μM) half an hour before 10 μM ketamine treatment in neuronal cultures and 2 mM ketamine treatment in neuron–glia mixed cultures for 24 h. Different doses of ketamine chosen in neuronal cultures and neuron–glia mixed cultures are based on the results of cell viability tests[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][3]

Rats: 2-PMPA is dissovled in methanol and diluted in acetonitrile/water (1:1, v/v). The concentration of stock solution is 1 mg/mL. Male Wistar rats are used in the study. 2-PMPA is administered to male Wistar rats as a single intraperitoneal (i.p.) dose. At 0.08, 0.25, 0.5, 1, 2, and 4 h post dose, blood samples are collected in heparinized microtubes by cardiac puncture immediately before sacrifice. Tissues (brains, sciatic nerves and DRG’s) are dissected after exsanguination and immediately flash frozen (-80°C). Plasma is prepared by centrifugation immediately after collection of blood samples. 2-PMPA is assayed in plasma and tissues by the developed LC/MS/MS method[1].

Mice: Male Swiss-Webster (SW) mice are used in the study. The effect of 2-PMPA is tested on an arbitrarily selected experimental group of 12 mice (group B) by injectingthe drug intraperitoneally (i.p.) at 80 mg/kg. The control group (group A) is injected i.p. with the water vehicle. Rotarod tests are then performed at additional times of 70, 240, 420, and 1440 min postinjection, and performance is measured as latency to fall, in seconds, at the tested rpm. A total of 480 2-min Rotarod tests are performed in this experiment[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 4.4224 mL 22.1122 mL 44.2243 mL 110.5608 mL
5 mM 0.8845 mL 4.4224 mL 8.8449 mL 22.1122 mL
10 mM 0.4422 mL 2.2112 mL 4.4224 mL 11.0561 mL
15 mM 0.2948 mL 1.4741 mL 2.9483 mL 7.3707 mL
20 mM 0.2211 mL 1.1056 mL 2.2112 mL 5.5280 mL
25 mM 0.1769 mL 0.8845 mL 1.7690 mL 4.4224 mL
30 mM 0.1474 mL 0.7371 mL 1.4741 mL 3.6854 mL
40 mM 0.1106 mL 0.5528 mL 1.1056 mL 2.7640 mL
50 mM 0.0884 mL 0.4422 mL 0.8845 mL 2.2112 mL
60 mM 0.0737 mL 0.3685 mL 0.7371 mL 1.8427 mL
80 mM 0.0553 mL 0.2764 mL 0.5528 mL 1.3820 mL
100 mM 0.0442 mL 0.2211 mL 0.4422 mL 1.1056 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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2-PMPA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

2-PMPA173039-10-62-(Phosphonomethyl)pentanedioic acidCarboxypeptidaseInhibitorinhibitorinhibit

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