CCR2-RA-[R] (C09-1120-625)

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC 50 of 103 nM.In VitroThe 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 [ 125 I]CCL2 from CCR2 with an pIC 50 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. 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”. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:CCR2 103 nM (IC 50 , in U2OS-CCR2 cells). Specification: 0.98 Molecular Formula: C18H19ClFNO3 Molecular Weight: 351.8 PubChem CID: 12093170 Isomeric SMILES: CC(=O)C1=C(C(=O)N([C@@H]1C2CCCCC2)C3=C(C=C(C=C3)Cl)F)O