Home / Chemokine Receptor Antagonists / J 113863

J 113863

Catalog #: 2595
4 Citations Datasheet
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J 113863 | CAS No. 202796-41-6 | Chemokine Receptor Antagonists
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Description: Potent CCR1 chemokine receptor antagonist

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%

Product Details
Citations (4)
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Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

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

M.Wt:
655.44
Formula:
C30H37Cl2IN2O2
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
202796-41-6

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

Other Product-Specific Information:

Background References

  1. 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.
  2. Design, synthesis, and discovery of a novel CCR1 antagonist.
    Naya et al.
    J.Med.Chem., 2001;44:1429
  3. Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo.
    Amat et al.
    Br.J.Pharmacol., 2006;149:666

Product Datasheets

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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

  1. 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
  2. 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
  3. PGC-1α induces SPP1 to activate macrophages and orchestrate functional angiogenesis in skeletal muscle.
    Authors: Rowe Et al.
    Circ Res  2014;115:504
  4. 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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