2-PCCA(hydrochloride)
目录号 : GC34382
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。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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-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.
| Cas No. | SDF | ||
| Canonical 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 |
| 溶解度 | DMSO : 100 mg/mL (203.21 mM; Need ultrasonic); H2O : 20 mg/mL (40.64 mM; Need ultrasonic) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0161 mL | 5.0803 mL | 10.1606 mL |
| 5 mM | 0.2032 mL | 1.0161 mL | 2.0321 mL |
| 10 mM | 0.1016 mL | 0.508 mL | 1.0161 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。