| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
2-MPPA targets glutamate carboxypeptidase II (GCP II), also known as NAALADase. GCP II is a metalloprotease involved in the hydrolysis of the neurotransmitter N-acetylaspartylglutamate (NAAG) to N-acetylaspartate (NAA) and glutamate. By inhibiting GCP II, 2-MPPA modulates glutamatergic neurotransmission. It is selective for GCP II over NMDA, kainate, and AMPA glutamate receptors, as well as over MMP-1, -2, -3, -7, -9, ACE, and NEP metalloproteases.
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| ln Vitro |
2-MPPA is a potent inhibitor of GCP II, with an IC50 of 90 nM. Its activity is typically measured by its ability to inhibit the hydrolysis of a substrate, such as N-acetylaspartylglutamate (NAAG), by the GCP II enzyme. In vitro, 2-MPPA (1-20 μM) has no effect on the intrinsic membrane properties of CA3 pyramidal neurons recorded in whole-cell current-clamp or voltage-clamp mode.
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| ln Vivo |
2-MPPA (10, 30, or 100 mg/kg) significantly reduced the prepulse inhibition (PPI) deficit in mice generated by dizocilpine (0.1 mg/kg) in a dose-dependent manner. Pretreatment with LY341495 (1.0 mg/kg), a selective group II metabotropic glutamate receptor (mGluR) antagonist, greatly counteracted the effects of 2-MPPA on dizocilpine-induced PPI insufficiency [1]. 2- The administration of 30 mg/kg of MPPA significantly reduced the incidence of SNCV defects caused by 5 mg/kg and 25 mg/kg of paclitaxel by 96.3 ± 4.4% and 98.3 ± 11.6%, respectively [2]. 2-In the high-expression PSMA model CWR22RS, 10-MPPA (10 mg/kg) suppresses tumor growth by 70% [2].
In vivo, 2-MPPA is orally bioavailable. It has demonstrated antinociceptive effects in a rat model of neuropathic pain and protects against motor neuron death in familial amyotrophic lateral sclerosis (ALS) mice. In mice, 2-MPPA (30 mg/kg, i.p.) increased jumping behavior in morphine-dependent mice and caused teeth chattering episodes. It also significantly attenuated dizocilpine-induced PPI deficits in a dose-dependent manner (10, 30, or 100 mg/kg, p.o.). |
| Enzyme Assay |
Non-cellular assays for 2-MPPA typically involve measuring its inhibition of GCP II enzyme activity. In a typical assay, purified GCP II enzyme is incubated with a substrate, such as NAAG or a synthetic analog, and varying concentrations of 2-MPPA. The production of glutamate is measured, and the IC50 is calculated.
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| Cell Assay |
In vitro cellular assays for 2-MPPA are not standardly described. Its primary characterization is based on enzyme inhibition assays.
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| Animal Protocol |
In vivo animal studies for 2-MPPA have been conducted in various models. It has shown antinociceptive effects in a rat model of neuropathic pain and protects against motor neuron death in familial ALS mice. In mice, it has been used to study opioid dependence and PPI deficits.
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| ADME/Pharmacokinetics |
2-MPPA is orally bioavailable. It has a molecular weight of 206.26. It is soluble in water (8 mg/mL) and DMSO (80 mg/mL).
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| Toxicity/Toxicokinetics |
Specific toxicological data for 2-MPPA are limited. As a research compound, comprehensive toxicity profiles are not typically available. It is intended for research use only and not for human therapeutic use.
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| References |
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| Additional Infomation |
2-MPPA is a research-grade compound for laboratory use only and is not approved for clinical use. Its primary application is in neuroscience research to study the role of GCP II in glutamatergic neurotransmission and to evaluate its potential as a therapeutic target for neurological disorders.
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| Molecular Formula |
C8H14O4S
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|---|---|
| Molecular Weight |
206.25936
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| Exact Mass |
206.061
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| CAS # |
254737-29-6
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| PubChem CID |
10198171
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| Appearance |
Colorless to light yellow ointment
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| LogP |
1.262
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
13
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| Complexity |
181
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(CC(CCC(=O)O)C(=O)O)CS
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| InChi Key |
FNLNSQHJKVQCBP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H14O4S/c9-7(10)4-3-6(8(11)12)2-1-5-13/h6,13H,1-5H2,(H,9,10)(H,11,12)
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| Chemical Name |
2-(3-sulfanylpropyl)pentanedioic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~484.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (12.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8482 mL | 24.2412 mL | 48.4825 mL | |
| 5 mM | 0.9697 mL | 4.8482 mL | 9.6965 mL | |
| 10 mM | 0.4848 mL | 2.4241 mL | 4.8482 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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