J 113863

Cat. No. 2595

J 113863 C30H37Cl2IN2O2 [353791-85-2]

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Chemical Name: 1,4-cis-1-(1-Cycloocten-1-ylmethyl)-4-[[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino]-1-ethylpiperidinium iodide

Biological Activity

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 of UCB 35625 (Cat. No. 2757).

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:
353791-85-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Amat et al (2006) Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo. Br.J.Pharmacol. 149 666. PMID: 17016504.

Naya et al (2001) Design, synthesis, and discovery of a novel CCR1 antagonist. J.Med.Chem. 44 1429. PMID: 11311066.

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Citations are publications that use Tocris products. Selected citations for J 113863 include:

Kamata et al (2015) The cholesterol-binding protein NPC2 restrains recruitment of stromal macrophage-lineage cells to early-stage lung tumours. Biomaterials 7 1119. PMID: 26183450.

Rowe et al (2014) PGC-1α induces SPP1 to activate macrophages and orchestrate functional angiogenesis in skeletal muscle. Circ Res 115 504. PMID: 25009290.

Gibon et al (2012) Effect of a CCR1 receptor antagonist on systemic trafficking of MSCs and polyethylene particle-associated bone loss. ScientificWorldJournal 33 3632. PMID: 22364730.

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Keywords: J 113863, supplier, Potent, CCR1, chemokine, receptor, antagonists, CXCR, Receptors, J113863, Rantes, Tocris Bioscience, Chemokine CC Receptor Antagonist products

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