2-PCCA HCl is a racemate and a GPR88 receptor agonist. It can inhibit GPR88-mediated cAMP production in HEK293 cells with EC50 of 116 nM.

Physicochemical Properties

Molecular Formula	C30H38CLN3O
Molecular Weight	492.10
Related CAS #	(1R,2R)-2-PCCA hydrochloride;1609563-71-4
Appearance	White to light yellow solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	EC50: 116 nM (GPR88 receptor, HEK293 cells)[1]
ln Vitro	2-PCCA hydrochloride, with an EC50 of 116 nM in HEK293 cells that stably express the human GPR88 receptor and the GloSensor-22F cAMP construct, inhibits GPR88-mediated cAMP generation via a Gαi-coupled pathway[2].
ln Vivo	2-PCCA (0.1-3.2 mg/kg, ip) reduces rat locomotor activity in a way that is dose-dependent. 2-PCCA also dose-dependently lessens methamphetamine-induced hyperactivity when paired with 1.0 mg/kg methamphetamine. 2-When tested in combination, PCCA (1-3.2 mg/kg, ip) neither produces nor modifies the discriminative stimulus effects of methamphetamine that are similar to those of methamphetamine[1].
References	[1]. 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]. 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.

Solubility Data

Solubility (In Vitro)

DMSO :~100 mg/mL (~203.21 mM) H2O :~20 mg/mL (~40.64 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0321 mL	10.1605 mL	20.3211 mL
	5 mM	0.4064 mL	2.0321 mL	4.0642 mL
	10 mM	0.2032 mL	1.0161 mL	2.0321 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.