2. Metabolic Enzyme/Protease
  3. Carboxypeptidase
  4. 2-PMPA

2-PMPA  (Synonyms: 2-(Phosphonomethyl)pentanedioic acid)

目录号: HY-100788 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

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。

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2-PMPA Chemical Structure

2-PMPA Chemical Structure

CAS No. : 173039-10-6

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ￥847
In-stock
1 mg ￥300
In-stock
5 mg ￥770
In-stock
10 mg ￥1210
In-stock
25 mg ￥2420
In-stock
50 mg ￥3520
In-stock
100 mg ￥5720
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of 2-PMPA:

2-PMPA 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

2-PMPA is a potent and selective inhibitor of glutamate carboxypeptidase II (GCPII) with an IC50 of 300 pM.

IC50 & Target

IC50: 300 pM (GCPII)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
LNCaP IC50
1.1 nM
Compound: 7, 2-PMPA
Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid scintillation counting
Inhibition of NAALADase activity in human LNCaP cell membranes assessed as inhibition of [3H]NAG conversion to [3H]glutamate after 30 mins by liquid scintillation counting
[PMID: 23025786]
体外研究
(In Vitro)

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

2-PMPA 相关抗体:
体内研究
(In Vivo)

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 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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

226.12

Formula

C6H11O7P
CAS 号
性状

固体

颜色

Light green to green

中文名称

2-(膦酰基甲基)戊二酸
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验： 

H2O 中的溶解度 : ≥ 28 mg/mL (123.83 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.4224 mL 22.1122 mL 44.2243 mL
5 mM 0.8845 mL 4.4224 mL 8.8449 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂： PBS

    Solubility: 100 mg/mL (442.24 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥98.0%

COA (284 KB) HNMR (247 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][3]

Rats: 2-PMPA is dissovled in methanol and diluted in acetonitrile/water (1:1, v/v). The concentration of stock solution is 1 mg/mL. Male Wistar rats are used in the study. 2-PMPA is administered to male Wistar rats as a single intraperitoneal (i.p.) dose. At 0.08, 0.25, 0.5, 1, 2, and 4 h post dose, blood samples are collected in heparinized microtubes by cardiac puncture immediately before sacrifice. Tissues (brains, sciatic nerves and DRG’s) are dissected after exsanguination and immediately flash frozen (-80°C). Plasma is prepared by centrifugation immediately after collection of blood samples. 2-PMPA is assayed in plasma and tissues by the developed LC/MS/MS method[1].

Mice: Male Swiss-Webster (SW) mice are used in the study. The effect of 2-PMPA is tested on an arbitrarily selected experimental group of 12 mice (group B) by injectingthe drug intraperitoneally (i.p.) at 80 mg/kg. The control group (group A) is injected i.p. with the water vehicle. Rotarod tests are then performed at additional times of 70, 240, 420, and 1440 min postinjection, and performance is measured as latency to fall, in seconds, at the tested rpm. A total of 480 2-min Rotarod tests are performed in this experiment[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

2-PMPA 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 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
15 mM 0.2948 mL 1.4741 mL 2.9483 mL 7.3707 mL
20 mM 0.2211 mL 1.1056 mL 2.2112 mL 5.5280 mL
25 mM 0.1769 mL 0.8845 mL 1.7690 mL 4.4224 mL
30 mM 0.1474 mL 0.7371 mL 1.4741 mL 3.6854 mL
40 mM 0.1106 mL 0.5528 mL 1.1056 mL 2.7640 mL
50 mM 0.0884 mL 0.4422 mL 0.8845 mL 2.2112 mL
60 mM 0.0737 mL 0.3685 mL 0.7371 mL 1.8427 mL
80 mM 0.0553 mL 0.2764 mL 0.5528 mL 1.3820 mL
100 mM 0.0442 mL 0.2211 mL 0.4422 mL 1.1056 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

2-PMPA173039-10-62-(Phosphonomethyl)pentanedioic acid2-(膦酰基甲基)戊二酸CarboxypeptidaseInhibitorinhibitorinhibit

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