| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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PMPA free acid is a novel and potent NAALADase inhibitor as well as a glutamate carboxypeptidase II (GCPII) inhibitor with IC50 of 300 pM.
| ln Vitro |
2-PMPA is a strong and specific GCPII inhibitor that catabolizes the neuropeptide N-acetylaspartylglutamate (NAAG), which is widely distributed, into N-acetylaspartate (NAA) and glutamine acid enzyme. 2. In numerous animal models of neurological disorders, 2-PMPA shows significant efficacy. 2. The analysis of biological matrices is severely hampered by 2-PMPA, a highly polar compound with numerous negative charges [1]. 2. In mixed cultures, PMPA mitigates the ketamine-induced reduction in cell viability and elevation in LDH levels, but not in neuronal cultures [2].
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| ln Vivo |
The maximal plasma concentration was observed after 0.25 hours following intraperitoneal dose of 100 mg/kg 2-PMPA, which was 275 μg/mL. The distribution volume, apparent clearance rate, half-life, area under the curve, and 7.93 mL/min/kg are, in that order, 0.44 L/kg, 210 μg×h/mL, and 0.64 h, respectively [1]. Following an initial increase in 2-PMPA at a dose of 250 mg/kg in mice under anesthesia, the gray matter BOLD signal rapidly declined and became much weaker. The gray matter brain T2* signals exhibit notable initial rises lasting several minutes at 167 and 250 mg/kg of 2-PMPA [3]. 2. In animal models of stroke and CCI, 2-PMPA has neuroprotective and anti-allodynia effects. A mean peak 2-PMPA concentration of 29.66±8.1 μM was obtained with administration of 50 mg/kg of 2-PMPA. This concentration shows great brain penetration, as it is around 100,000 times more than what is needed to inhibit NAAG peptidase. After 50 mg/kg 2-PMPA (ip) is administered, extracellular NAAG concentrations rise steadily and start to rise right away [4].
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| References |
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| Molecular Formula |
C6H11O7P
|
|---|---|
| Molecular Weight |
226.121103525162
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| Exact Mass |
226.024
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| CAS # |
173039-10-6
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| Related CAS # |
373645-42-2 (sodium);173039-10-6 (free acid);
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| PubChem CID |
10130754
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| Appearance |
Light yellow to yellow ointment
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
538.8±60.0 °C at 760 mmHg
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| Flash Point |
279.6±32.9 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.541
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| LogP |
-2.85
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
14
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| Complexity |
267
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC(CCC(CP(=O)(O)O)C(=O)O)=O
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| InChi Key |
ISEYJGQFXSTPMQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H11O7P/c7-5(8)2-1-4(6(9)10)3-14(11,12)13/h4H,1-3H2,(H,7,8)(H,9,10)(H2,11,12,13)
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| Chemical Name |
2-(phosphonomethyl)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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O : ≥ 28 mg/mL (~123.83 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (442.24 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4422 mL | 2.2112 mL | 4.4224 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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