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

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

Cat. No.: HY-100788 Purity: 98.0%
Handling Instructions Technical Support

2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA is applicable to the research of neurological diseases.

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

CAS No. : 173039-10-6

Size Price Stock Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of 2-PMPA:

Top Publications Citing Use of Products

    2-PMPA purchased from MedChemExpress. Usage Cited in: ACS Nano. 2021 Apr 27;15(4):7179-7194.  [Abstract]

    After incubation with 2-PMPA (0.5 mM; 6 h), the uptake of Fluoro-GBP@Fe3O4 (50 μg Fe/mL) in C4-2 cells was assessed by flow cytometry.

    2-PMPA purchased from MedChemExpress. Usage Cited in: ACS Nano. 2021 Apr 27;15(4):7179-7194.  [Abstract]

    2-PMPA (0.5 μM; i.v.; 1-6 h) obviously inhibited the gradual aggregation of GBP@Fe3O4 at the tumor sites in C4-2 tumor-bearing mice.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA is applicable to the research of neurological diseases[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    LNCaP IC50
    1.1 nM
    Compound: 7, 2-PMPA
    Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid scintillation counting
    Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid scintillation counting
    [PMID: 23025786]
    LNCaP IC50
    52 nM
    Compound: PMPA
    Displacement of [125I]23 from PSMA in human LNCAP cells
    Displacement of [125I]23 from PSMA in human LNCAP cells
    [PMID: 26894427]
    In Vitro

    2-PMPA remains stable in rat plasma when stored at room temperature for 4 h, subjected to 3 freeze-thaw cycles, stored at -80°C for 28 days, and placed in a 10°C autosampler for 18 h[2].

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

    In Vivo

    2-PMPA (167-250 mg/kg; intraperitoneal injection; single dose) induces a dose-dependent biphasic BOLD signal response in the gray matter of anesthetized mice, with a sustained signal decrease of 2.15-4.64% at 250 mg/kg and a transient signal decrease of 1% at 167 mg/kg[1].
    2-PMPA (80 mg/kg; i.p.; single dose) exerts no significant effects on motor coordination or cognitive ability in Swiss-Webster mice within 24 hours[1].
    2-PMPA (100 mg/kg; intraperitoneal injection; single dose) is rapidly absorbed in male Wistar rats, with low brain penetration (a brain/plasma AUC0-t ratio of 0.018), while it shows higher penetration in peripheral nerve tissues[2].

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

    Animal Model: Swiss-Webster (SW) (male, approx 6-8 wk old)[2]
    Dosage: 80 mg/kg
    Administration: i.p.; single dose
    Result: Showed mean latency to fall not significantly different from control mice at all tested time points (70, 240, 420, 1440 min post-administration).
    Caused no impairment in motor coordination or cognitive ability observed over the 24-h period.
    Molecular Weight

    226.12

    Formula

    C6H11O7P

    CAS No.
    Appearance

    Oil

    Color

    Off-white to light 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, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (442.24 mM; Need ultrasonic)

    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, away from moisture). 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

    Purity: 98.0%

    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, away from moisture). 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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    • 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.

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    Product Name:
    2-PMPA
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