PMPA(NAALADaseinhibitor)
- CAS No.173039-10-6
- Chemical Name:PMPA(NAALADaseinhibitor)
- CBNumber:CB91075110
- Molecular Formula:C6H11O7P
- Formula Weight:226.12
- MOL File:173039-10-6.mol
- Boiling point 538.8±60.0 °C(Predicted)
- Density 1.658±0.06 g/cm3(Predicted)
- storage temp. room temp
- solubility Soluble to 100 mM in sterile
- pka 2.06±0.10(Predicted)
- form powder
- color white to beige
- Water Solubility Soluble to 100 mM in water
- FDA UNII XH88WJG9LJ
- UNSPSC Code 12352200
- NACRES NA.77
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H315-H319
- Precautionary statements P305+P351+P338
- Brand: Sigma-Aldrich(India)
- Product number: SML1612
- Product name : 2-PMPA
- Purity: ≥98% (HPLC)
- Packaging: 5MG
- Price: ₹12308.03
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: SML1612
- Product name : 2-PMPA
- Purity: ≥98% (HPLC)
- Packaging: 25MG
- Price: ₹49578.5
- Updated: 2022/06/14
- Buy: Buy
PMPA(NAALADaseinhibitor) Chemical Properties,Usage,Production
- Uses 2-(Phosphonomethyl)pentanedioic Acid is a selective glutamate carboxypeptidase 2 (GCP-II) inhibitor, the enzyme which catabolizes the abundant neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to N-acetylaspartate (NAA) and glutamate. A posiible target in the treatment of multiple sclerosis and Schizophrenia.
- Biological Activity Highly potent and selective inhibitor of? glutamate carboxypeptidase 2 (GCP II/N-acetylated α -linked dipeptidase/NAALADase) with a K i value of 275 pM. Neuroprotective; protects against glutamate-mediated motor neuron degeneration and reduces volume of injury following middle cerebral artery occlusion (MCAO).
- Biochem/physiol Actions 2-PMPA is a potent and selective inhibitor of Glutamate carboxypeptidase II (GCPII).
-
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].
- storage Desiccate at RT
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- 抑制剂
- 高端化学
- 2-(膦酸基甲基)戊二酸
- 2-PMPA游离态
- 化合物2-PMPA
- 2-(膦酰基甲基)戊二酸
- NAALADASEINHIBITOR(易潮)
- 173039-10-6
- inhibit,Inhibitor,2PMPA,Carboxypeptidase,2-PMPA,2 PMPA
- 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID (PMPA)
- Pentanedioic acid, 2-(phosphonomethyl)-
- NAALADASEINHIBITOR
- 2-PMPA(NAALADaseinhibitor)
- CS-2454
- 2-PMPA
- 2-(Phosphonomethyl)pentane-1,5-dioicacid
- PMPA(NAALADaseinhibitor)