2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID
中文名称 | 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID |
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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
沸点 | 538.8±60.0 °C(Predicted) |
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密度 | 1.658±0.06 g/cm3(Predicted) |
储存条件 | room temp |
溶解度 | 无菌条件下可溶至 100 mM |
酸度系数(pKa) | 2.06±0.10(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
水溶解性 | Soluble to 100 mM in water |
IC50: 300 pM (GCPII)
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.
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
RTECS号 | SA0454800 |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-100788 | 2-PMPA | 1 mg | 300元 | |
2024/08/19 | HY-100788 | 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 2-PMPA | 173039-10-6 | 5mg | 770元 |