J 113863
Chemical Name: 1,4-cis-1-(1-Cycloocten-1-ylmethyl)-4-[[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino]-1-ethylpiperidinium iodide
Purity: ≥98%
Biological Activity
J 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.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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PGC-1alpha induces SPP1 to activate macrophages and orchestrate functional angiogenesis in skeletal muscle.
Rowe G, Raghuram S, Jang C, Nagy J, Patten I, Goyal A, Chan M, Liu L, Jiang A, Spokes K, Beeler D, Dvorak H, Aird W, Arany Z
Circ Res, 2014;115(5):504-17. -
Design, synthesis, and discovery of a novel CCR1 antagonist.
Naya et al.
J.Med.Chem., 2001;44:1429 -
Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo.
Amat et al.
Br.J.Pharmacol., 2006;149:666
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Citations for J 113863
The citations listed below are publications that use Tocris products. Selected citations for J 113863 include:
4 Citations: Showing 1 - 4
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CCR1 antagonist J-113863 corrects the imbalance of pro- and anti-inflammatory cytokines in a SJL/J mouse model of relapsing-remitting multiple sclerosis.
Authors: Ansari Et al.
Immunobiology 2022;227:152245
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The cholesterol-binding protein NPC2 restrains recruitment of stromal macrophage-lineage cells to early-stage lung tumours.
Authors: Kamata Et al.
Biomaterials 2015;7:1119
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PGC-1α induces SPP1 to activate macrophages and orchestrate functional angiogenesis in skeletal muscle.
Authors: Rowe Et al.
Circ Res 2014;115:504
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Effect of a CCR1 receptor antagonist on systemic trafficking of MSCs and polyethylene particle-associated bone loss.
Authors: Gibon Et al.
ScientificWorldJournal 2012;33:3632
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