CCR2 antagonist 4

Research use only, not for human use.

CCR2 antagonist 4 is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM).

CCR2 antagonist 4 is a potent and specific antagonist of CCR2(IC50s of 180 nM), and potently inhibits MCP-1-induced chemotaxis(IC50 of 24 nM).(In Vivo):Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta in ApoE-deficient mice.

Ile263 and Thr292 in CCR2 contribute significantly to binding of Teijin compound 1 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, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with CCR2 antagonist 4.In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta.

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Teijin compound 1

Autophagy

CCR

G. candidum histidinol dehydrogenase

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226226-39-7

439.86

C21H21ClF3N3O2

>98% (HPLC)

In Vitro:?DMSO : ≥ 50 mg/mL (113.67 mM)

FC(F)(F)c1cccc(c1)C(=O)NCC(=O)N[C@@H]1CCN(Cc2ccc(Cl)cc2)C1

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(-20℃)

With Ice Pack

≥ 2 years