Powder: -20°C for 3 years | In solvent: -80°C for 1 year
2-PMPA (2-(Phosphonomethyl)pentanedioic acid) 是谷氨酸羧肽酶II 的选择性抑制剂(IC50:300 pM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 293 | 现货 | ||
5 mg | ¥ 688 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 2,660 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,680 | 现货 |
产品描述 | 2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) (IC50=300 pM). |
靶点活性 | GCP II:300 pM |
体外活性 | 2-PMPA is a potent and selective inhibitor of GCPII. GCPII is an enzyme that 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[1]. 2-PMPA reduces ketamine-induced decrease of cell viability and increase of LDH levels in the mixed cultures but not in the neuronal cultures[2]. |
体内活性 | 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 exhibits neuroprotective activity in an animal model of stroke and anti-allodynic activity in CCI model. Administration of 2-PMPA (50 mg/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 suggests extremely 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]. |
细胞实验 | Neuronal cultures and neuron–glia mixed cultures are treated with ketamine diluted in the culture medium (1, 3, 10, 30, 100, 300, 1000, 2000, 3000 μM) for 24 h to compare neurotoxicity in these two different cell cultures. 2-PMPA is selected to explore the protective effect on ketamine-induced neurotoxicity in these two different cell cultures. Cells are exposed to 2-PMPA (20, 50, 100 μM) half an hour before 10 μM ketamine treatment in neuronal cultures and 2 mM ketamine treatment in neuron–glia mixed cultures for 24 h. Different doses of ketamine chosen in neuronal cultures and neuron–glia mixed cultures are based on the results of cell viability tests[2]. |
别名 | 2-(Phosphonomethyl)pentanedioic acid |
分子量 | 226.12 |
分子式 | C6H11O7P |
CAS No. | 173039-10-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 28 mg/mL (123.83 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 4.4224 mL | 22.1122 mL | 44.2243 mL | 110.5608 mL |
5 mM | 0.8845 mL | 4.4224 mL | 8.8449 mL | 22.1122 mL | |
10 mM | 0.4422 mL | 2.2112 mL | 4.4224 mL | 11.0561 mL | |
20 mM | 0.2211 mL | 1.1056 mL | 2.2112 mL | 5.528 mL | |
50 mM | 0.0884 mL | 0.4422 mL | 0.8845 mL | 2.2112 mL | |
100 mM | 0.0442 mL | 0.2211 mL | 0.4422 mL | 1.1056 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
2-PMPA 173039-10-6 Proteases/Proteasome Carboxypeptidase 2-(Phosphonomethyl)pentanedioic acid inhibit Inhibitor 2PMPA 2 PMPA inhibitor