2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID

生物活性靶點(diǎn)體外研究體內(nèi)研究 用途與合成方法 MSDS 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID價(jià)格(試劑級(jí)) 上下游產(chǎn)品信息

中文名稱	2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID
中文同義詞	NAALADASEINHIBITOR(易潮);2-(膦?；谆?戊二酸;化合物2-PMPA;2-PMPA游離態(tài);2-(膦酸基甲基)戊二酸
英文名稱	PMPA(NAALADaseinhibitor)
英文同義詞	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號(hào)	173039-10-6
分子式	C6H11O7P
分子量	226.12
EINECS號(hào)
相關(guān)類別
Mol文件	173039-10-6.mol
結(jié)構(gòu)式

2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 性質(zhì)

2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 用途與合成方法

生物活性

2-PMPA是高效選擇性的谷氨酸羧肽酶II (GCPII)抑制劑，IC50值為300 pM。

靶點(diǎn)

IC50: 300 pM (GCPII)

體外研究

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.

體內(nèi)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 價(jià)格(試劑級(jí))

2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 上下游產(chǎn)品信息