CCR2-RA-[R]

512177-83-2

C18H19ClFNO3

DMSO : >= 125 mg/mL (355.32 mM); H2O : < 0.1 mg/mL (insoluble)

Immunology/Inflammation; GPCR/G Protein

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC₅₀ of 103 nM. IC50 & Target: IC50: 103 nM (CCR2)^[1] In Vitro: The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. CCR2-RA-[R] displaces [¹²⁵I]CCL2 from CCR2 with an pIC₅₀ value of 6.1. The pK_D of CCR2-RA-[R] for CCR2 and CCR5 is 8.8+/-0.1 and 7.0+/-0.1, respectively^[2]. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket "druggability"^[3].