2-PCCA hydrochloride
Based on 1 Customer Validation
2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
For research use only. We do not sell to patients.
- Purity: 99.11%
- Formula: C30H38ClN3O
- Molecular Weight:492.10
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
EC50: 116 nM (GPR88 receptor, HEK293 cells)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 492.10
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Formula C30H38ClN3O
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Color White to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL (203.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 20 mg/mL (40.64 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.0321 mL | 10.1605 mL | 20.3211 mL | 50.8027 mL |
| 5 mM | 0.4064 mL | 2.0321 mL | 4.0642 mL | 10.1605 mL | |
| 10 mM | 0.2032 mL | 1.0161 mL | 2.0321 mL | 5.0803 mL | |
| 15 mM | 0.1355 mL | 0.6774 mL | 1.3547 mL | 3.3868 mL | |
| 20 mM | 0.1016 mL | 0.5080 mL | 1.0161 mL | 2.5401 mL | |
| 25 mM | 0.0813 mL | 0.4064 mL | 0.8128 mL | 2.0321 mL | |
| 30 mM | 0.0677 mL | 0.3387 mL | 0.6774 mL | 1.6934 mL | |
| 40 mM | 0.0508 mL | 0.2540 mL | 0.5080 mL | 1.2701 mL | |
| DMSO | 50 mM | 0.0406 mL | 0.2032 mL | 0.4064 mL | 1.0161 mL |
| 60 mM | 0.0339 mL | 0.1693 mL | 0.3387 mL | 0.8467 mL | |
| 80 mM | 0.0254 mL | 0.1270 mL | 0.2540 mL | 0.6350 mL | |
| 100 mM | 0.0203 mL | 0.1016 mL | 0.2032 mL | 0.5080 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.