(1R,2R)-2-PCCA hydrochloride_product_DataBase

Bioactivity	(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
Target	EC50: 3 nM (GPR88 receptor), 603 nM (GPR88 receptor, in GPR88-22F cells)
Invitro	(1R,2R)-2-PCCA (Example 3) is a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay[1][2]. (1R,2R)-2-PCCA inhibits GPR88-mediated cAMP production through a Gαi-coupled pathway, with an EC50 of 56 nM in HEK293 cells stably expressing the human GPR88 receptor and the GloSensor-22F cAMP construct[2].
Name	(1R,2R)-2-PCCA hydrochloride
CAS	1609563-71-4
Formula	C30H39Cl2N3O
Molar Mass	528.56
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Reference	[1]. Bi, Yingzhi, et al. Modulators of G Protein-Coupled Receptor 88. US 20110251204 A1. [2]. Jin C, et al. Synthesis, pharmacological characterization, and structure-activity relationship studies of small molecular agonists for the orphan GPR88 receptor. ACS Chem Neurosci. 2014 Jul 16;5(7):576-87. [3]. 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.

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