Description | (1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice.(1R,2R)-2-PCCA hydrochloride can be used to study the central nervous system. |
In vitro | (1R,2R)-2-PCCA hydrochloride 是一种有效的GPR88受体激动剂,在无细胞实验中具有3 nM的EC50,而在细胞实验中EC50为603 nM[1]。通过Gαi耦联途径,(1R,2R)-2-PCCA hydrochloride能够抑制GPR88介导的cAMP产生,在稳定表达人GPR88受体和GloSensor-22F的HEK293细胞中的cAMP构建物中EC50为56 nM[1]。 |
Target activity | GPR88-22F cells:603 nM (EC50), GPR88 receptor:3 nM (EC50, cell-free assay), GPR88 receptor:56 nM (EC50, HEK293 cell) |
Synonyms | (1R,2R)-2-PCCA(hydrochloride) |
molecular weight | 528.56 |
Molecular formula | C30H39Cl2N3O |
CAS | 1609563-71-4 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility | DMSO: 20 mg/mL (37.84 mM), Sonication is recommended. |
References | 1. 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. 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. |