Chemical Name: 1,4-cis-1-(1-Cycloocten-1-ylmethyl)-4-[[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino]-1-ethylpiperidinium iodide
Biological ActivityJ 113863 is a potent chemokine receptor 1 (CCR1) antagonist (IC50 values are 0.9 and 5.8 nM for human and mouse CCR1 receptors respectively). Also displays high selectivity for human but not mouse CCR3 receptors (IC50 values are 0.58 and 460 nM respectively). Improves paw inflammation, joint damage and dramatically reduces cell infiltration into joints in collagen-induced arthritis in mice.
Isomer also available.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Design, synthesis, and discovery of a novel CCR1 antagonist.
Naya et al.
Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo.
Amat et al.
Citations for J 113863
The citations listed below are publications that use Tocris products. Selected citations for J 113863 include:
3 Citations: Showing 1 - 3
The cholesterol-binding protein NPC2 restrains recruitment of stromal macrophage-lineage cells to early-stage lung tumours.
Authors: Kamata Et al.
PGC-1α induces SPP1 to activate macrophages and orchestrate functional angiogenesis in skeletal muscle.
Authors: Rowe Et al.
Circ Res 2014;115:504
Effect of a CCR1 receptor antagonist on systemic trafficking of MSCs and polyethylene particle-associated bone loss.
Authors: Gibon Et al.
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J113863 was used in a chemotaxis assay using a subset of C57Bl/6 splenic cells. Cells were pretreated with J113863 for 2 hours before being added to the top portion of a transwell assay. CCL6 or media was used and the chemoattractant and cells were given 2 hours to migrate.