2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID
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- CAS号:
- 173039-10-6
- 英文名:
- PMPA(NAALADaseinhibitor)
- 英文别名:
- 2-PMPA;CS-2454;NAALADASEINHIBITOR;PMPA(NAALADaseinhibitor);2-PMPA(NAALADaseinhibitor);Pentanedioic acid, 2-(phosphonomethyl)-;2-(Phosphonomethyl)pentane-1,5-dioicacid;2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID (PMPA);inhibit,Inhibitor,2PMPA,Carboxypeptidase,2-PMPA,2 PMPA
- 中文名:
- 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID
- 中文别名:
- 2-PMPA游离态;化合物2-PMPA;2-(膦酸基甲基)戊二酸;2-(膦酰基甲基)戊二酸;NAALADASEINHIBITOR(易潮)
- CBNumber:
- CB91075110
- 分子式:
- C6H11O7P
- 分子量:
- 226.12
- MOL File:
- 173039-10-6.mol
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2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID化学性质
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沸点:
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538.8±60.0 °C(Predicted)
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密度:
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1.658±0.06 g/cm3(Predicted)
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储存条件:
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room temp
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溶解度:
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Soluble to 100 mM in sterile
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酸度系数(pKa):
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2.06±0.10(Predicted)
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形态:
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powder
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颜色:
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white to beige
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水溶解性:
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Soluble to 100 mM in water
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2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID性质、用途与生产工艺
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。
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
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* 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.
2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/01/25 | HY-100788 | 2-PMPA | | 1 mg | 377元 |
2024/01/25 | HY-100788 | 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 2-PMPA | 173039-10-6 | 5mg | 830元 |
2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID
生产厂家
173039-10-6, 2-(PHOSPHONOMETHYL)PENTANEDIOIC ACID 相关搜索:
- 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)