2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID CAS#: 173039-10-6

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2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID价格(试剂级) 上下游产品信息

中文名称	2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID
中文同义词	NAALADASEINHIBITOR(易潮);2-(膦酰基甲基)戊二酸;化合物2-PMPA;2-PMPA游离态;2-(膦酸基甲基)戊二酸
英文名称	PMPA(NAALADaseinhibitor)
英文同义词	PMPA(NAALADaseinhibitor);2-(Phosphonomethyl)pentane-1,5-dioicacid;2-PMPA;CS-2454;2-PMPA(NAALADaseinhibitor);NAALADASEINHIBITOR;Pentanedioic acid, 2-(phosphonomethyl)-;2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID (PMPA)
CAS号	173039-10-6
分子式	C6H11O7P
分子量	226.12
EINECS号
相关类别
Mol文件	173039-10-6.mol
结构式

2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 性质

2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 用途与合成方法

生物活性

2-PMPA是高效选择性的谷氨酸羧肽酶II (GCPII)抑制剂，IC50值为300 pM。

靶点

IC50: 300 pM (GCPII)

体外研究

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. 2-PMPA reduces ketamine-induced decrease of cell viability and increase of LDH levels in the mixed cultures but not in the neuronal cultures.

体内研究

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. 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 T     ₂    * signals in gray matter at both 167 and 250 mg/kg includes a significant initial rise lasting several minutes. 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.

安全信息

MSDS信息

2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 价格(试剂级)

2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 上下游产品信息