CAM-IN-1

CAM-IN-1 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 values of 7 and 5 nM, respectively.

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

IC50: 7 nM (E-selectin), 5 nM (ICAM-1)[1]

CAM-IN-1 shows significant efficacy in a rat rheumatoid arthritis model and in a mouse asthma model. CAM-IN-1 reduces the width of inflamed ankles after the ninth day following treatment, but shows no efficacy in the acute phase. Treatment with CAM-IN-1 (25 mg/kg) for 21 days significantly reduces the ankle inflammation of the arthritis rats. Significant reduction of eosinophils and serum-soluble ICAM-1 (sICAM-1) is observed[1].

Rats: In a rat rheumatoid arthritis model, 26 all rats are treated with peptidoglycan polysaccharide to elicit the disease to a desired degree. Six rats per group are then treated with CAM-IN-1 or vehicle control twice daily. The ankles of these rats are measured on day 0, 1, 3, 7, 9, 11, 16, 18, and 21 after administration. Histologic analyses of the ankles are performed on the last day of the experiment[1].

[1]. Zhu GD, et al. Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Arylmodifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides. J Med Chem. 2001 Oct 11;44(21):3469-87.

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