CCR2 antagonist 4 hydrochlorideCCR2 antagonist 4 hydrochloride
MedChemExpress (MCE)
HY-103362
1313730-14-1
Teijin compound 1 hydrochloride
99.86%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
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.
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 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].
CCR2b 180 nM (IC50)
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[1]. Moree WJ, et al. Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series. Bioorg Med Chem Lett. 2008 Mar 15
18(6):1869-73. [Content Brief]
[2]. Hall SE, et al. Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol Pharmacol. 2009 Jun
75(6):1325-36. [Content Brief]
[3]. Calin M, et al. VCAM-1 directed target-sensitive liposomes carrying CCR2 antagonists bind to activated endothelium and reduce adhesion and transmigration of monocytes. Eur J Pharm Biopharm. 2015 Jan
89:18-29. [Content Brief]