2-PCCA(hydrochloride)

目录号: GC34382纯度: >99.50%

2-PCCAhydrochloride是一种外消旋体，为GPR88受体激动剂，在HEK293细胞中，可抑制GPR88介导的cAMP的产生，EC50值为116nM。

规格	价格	库存	数量
5mg	¥2,250.00	现货	1
10mg	¥4,050.00	现货	1
25mg	¥8,100.00	现货	1
50mg	¥12,600.00	现货	1
10mM (in 1mL DMSO)	询价	现货	1

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187(9):2288-2304 (2024)
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183(7):1867-1883 (2020)
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产品描述 Description

2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.

2-PCCA hydrochloride inhibits GPR88-mediated cAMP production through a Gαi-coupled pathway, with an EC50 of 116 nM in HEK293 cells stably expressing the human GPR88 receptor and the GloSensor-22F cAMP construct[2].

2-PCCA (0.1-3.2 mg/kg, i.p.) decreases the locomotor activity in rats in a dose-dependent manner in rats. 2-PCCA combined with 1.0 mg/kg methamphetamine also dose-dependently reduces methamphetamine-induced hyperactivity. 2-PCCA (1-3.2 mg/kg, i.p.) alone does not produce methamphetamine-like discriminative stimulus effects, or alter the discriminative stimulus effects of methamphetamine, when studied in combination[1].

[1]. Li JX, et al. The GPR88 receptor agonist 2-PCCA does not alter the behavioral effects of methamphetamine in rats. Eur J Pharmacol. 2013 Jan 5;698(1-3):272-7. [2]. Jin C, et al. Effect of Substitution on the Aniline Moiety of the GPR88 Agonist 2-PCCA: Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies. ACS Chem Neurosci. 2016 Oct 19;7(10):1418-1432.

实验参考方法 Experimental Reference Method

Animal experiment:

Rats[1]For the locomotor activity tests, rats are only used once. The test is conducted in an adjacent room from the animal colony room with similar environmental conditions (light, temperature and humidity). Before tests begin, rats are exposed to at least three days of handling by the experimenter. When only 2-PCCA (1.0 and 3.2 mg/kg) is studied, the drug is (i.p.) injected immediately before the rats are put into the test chambers and the locomotor activity is simultaneously recorded for 60 min. When 2-PCCA is studied in combination with methamphetamine, the locomotor activity is recorded for 20 min and then both drugs are simultaneously injected and the locomotor activity is recorded for 120 more min[1].

References:

[1]. Li JX, et al. The GPR88 receptor agonist 2-PCCA does not alter the behavioral effects of methamphetamine in rats. Eur J Pharmacol. 2013 Jan 5;698(1-3):272-7.
[2]. Jin C, et al. Effect of Substitution on the Aniline Moiety of the GPR88 Agonist 2-PCCA: Synthesis, Structure-Activity Relationships, and Molecular Modeling Studies. ACS Chem Neurosci. 2016 Oct 19;7(10):1418-1432.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

SMILES

[H]Cl.[H]Cl.CCCC1=CC=C(C2=CC=C(N(C[C@@H](N)[C@@H](C)CC)C([C@@H]3[C@@H](C4=CC=CC=N4)C3)=O)C=C2)C=C1.CCCC5=CC=C(C6=CC=C(N(C[C@@H](N)[C@@H](C)CC)C([C@H]7[C@H](C8=CC=CC=N8)C7)=O)C=C6)C=C5

分子式

C₆₀H₇₆Cl₂N₆O₂

分子量

984.19 g/mol

溶解性

DMSO : 100 mg/mL (203.21 mM; Need ultrasonic); H<sub>2</sub>O : 20 mg/mL (40.64 mM; Need ultrasonic)

保存条件

Store at -20°C

General tips

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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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