DL-AP3|cas:5652-28-8|西域试剂

DL-AP3

产品编号：Bellancom-100786| CAS NO：5652-28-8| 分子式：C₃H₈NO₅P| 分子量：169.07

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货号	价格	库存与货期
Bellancom-100786	￥400.00	杭州北京（现货）
Bellancom-100786	￥900.00	杭州北京（现货）
Bellancom-100786	￥1400.00	杭州北京（现货）

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DL-AP3

产品介绍

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。

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.

体外研究

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)。
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。
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，K_i 为 77 µM。
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)。

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

Cell Viability Assay

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

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。
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]。

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

Animal Model:	Fmr1 KO mice
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.

体内研究

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

Animal Model:	Fmr1 KO mice
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.

体内研究

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

Animal Model:	Fmr1 KO mice
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.

性状

Solid

溶解性数据

In Vitro:

H₂O : 5 mg/mL (29.57 mM; ultrasonic and warming and heat to 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

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。

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)

参考文献