DL-AP3

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DL-AP3  纯度: ≥98.0%

DL-AP3 是一种竞争性的 mGluR1 和 mGluR5 拮抗剂。DL-AP3 也是磷酸丝氨酸磷酸酶 (phosphoserine phosphatase) 的抑制剂。DL-AP3具有神经保护作用。

DL-AP3

DL-AP3 Chemical Structure

CAS No. : 5652-28-8

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DL-AP3 相关产品

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生物活性

DL-AP3 is a competitive mGluR1 and mGluR5 antagonist. DL-AP3 is also an inhibitor of phosphoserine phosphatase. DL-AP3 has neuroprotective effect[1][2][3].

IC50 & Target[1]

mGluR 1

 

mGluR 5

 

体外研究
(In Vitro)

DL-AP3 (10 µM，6 小时) 减轻原代神经元中氧-葡萄糖剥夺 (OGD) 引起的损伤 (细胞活力)[1]。
DL-AP3 (10 µM，6 小时) 恢复原代神经元中 OGD 诱导的 p-Akt1 水平降低和细胞色素 C 增加[1]。
DL-AP3 (1-100 µM) 抑制大鼠脑磷酸丝氨酸磷酸酶的活性，IC50 为 187 µM，Ki 为 77 µM[2]。
DL-AP3 (10 μM, 10min) 联合 SKF81297 (5 μM) 在 Fmr1 KO 小鼠的切片中诱导显著的的长时程增强 (LTP)[3]。

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

DL-AP3 相关抗体:

Cell Viability Assay[1]

Cell Line: Primary neurons with oxygen-glucose deprivation (OGD) treatment
Concentration: 10 µM
Incubation Time: 24 h or 72 h
Result: Attenuated the inhibitory effect of OGD on neuronal viability.

Western Blot Analysis[1]

Cell Line: Primary neurons with oxygen-glucose deprivation (OGD) treatment
Concentration: 10 µM
Incubation Time: 6 h
Result: Increased the decreased levels of p-Akt1, and decreased the increase of cytochrome C.

体内研究
(In Vivo)

DL-AP3 (4 mg/kg, i.p., 持续 5 周) 联合 SKF81297 (1 mg/kg, i.p.) 减少Fmr1 KO 小鼠多动表型[3]。
DL-AP3 (4.0-12.0 mg/animal, i.c.v. infusion, 100 μL) 阻断绵羊内脏痛症状的发展，以及血浆中神经内分泌学变化[4]。

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Fmr1 KO mice[3]
Dosage: 4 mg/kg with SKF81297 (1 mg/kg)
Administration: i.p., for 5 weeks.
Result: Reduced the distance traveled by Fmr1 KO mice (open-field test).
Reduced the swim latency on the final day in the Fmr1 KO mice (Morris Water Maze test).
Animal Model: Sheep with visceral pain evoked by colonic distension (CD)[4]
Dosage: 4.0-12.0 mg/animal
Administration: i.c.v. infusion, 100 μL
Result: Decreased intensity from appearance of clinical signs of visceral pain caused by CD test.
Diminished the increase of plasma cortisol, E, NE and DA concentrations caused by visceral pain provoked by CD episode.

分子量

169.07

Formula

C3H8NO5P
CAS 号

5652-28-8
性状

固体

颜色

White to off-white

结构分类
  • Others
初始来源
  • 内源性代谢物
运输条件

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

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O 中的溶解度 : 5 mg/mL (29.57 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.9147 mL 29.5735 mL 59.1471 mL
5 mM 1.1829 mL 5.9147 mL 11.8294 mL
10 mM 0.5915 mL 2.9574 mL 5.9147 mL

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* 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 (sealed storage, away from moisture)。-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。

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

质量

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浓度

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体积

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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

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体积 (final)

V2

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动物溶解方案

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

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工作液所需浓度 : mg/mL

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纯度 & 产品资料

纯度: ≥98.0%

Data Sheet (602 KB) SDS (251 KB)

COA (262 KB) HNMR (251 KB) CNMR (309 KB)

产品使用指南 (1538 KB)

参考文献

  • [1]. Cui D, et al. DL-2-amino-3-phosphonopropionic acid protects primary neurons from oxygen-glucose deprivation induced injury. Bosn J Basic Med Sci. 2017 Feb 21;17(1):12-16.  [Content Brief]

    [2]. Hawkinson JE, et al. The metabotropic glutamate receptor antagonist L-2-amino-3-phosphonopropionic acid inhibits phosphoserine phosphatase. Eur J Pharmacol. 1996 Jun 27;307(2):219-25.  [Content Brief]

    [3]. Xu ZH, et al. Group I mGluR antagonist rescues the deficit of D1-induced LTP in a mouse model of fragile X syndrome. Mol Neurodegener. 2012 May 28;7:24.  [Content Brief]

    [4]. B.F. Kania, et al. Supraspinal basis of analgesic and clinical effects of the metabotropic glutamate mGluR1 antagonist during colonic distension in sheep. Small Ruminant Research. 2014. 117 (1).

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