CCR2 antagonist 4 (hydrochloride)

1313730-14-1

476.32

DMSO : 250 mg/mL (524.86 mM; Need ultrasonic)

Immunology/Inflammation; GPCR/G Protein

CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC₅₀s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC₅₀ of 24 nM^[1]. In Vitro: Ile263 and Thr292 in CCR2 contribute significantly to binding of CCR2 antagonist 4 in CCR2. Residue Glu291 in TM7, a highly conserved residue in many CC chemokine receptors, contributes substantially to binding of the protonated CCR2 antagonist 4 hydrochloride, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with CCR2 antagonist 4 hydrochloride^[2]. In Vivo: In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 hydrochloride reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta^[3].