J 113863

Name: J 113863
Brand: Tocris Bioscience
SKU: 2595
Rating: 5 (1 reviews)

Catalog # 2595 | Tocris Bioscience a Bio-Techne Brand

(1)

Citations (4)

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Potent CCR1 chemokine receptor antagonist

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Key Product Details

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% (HPLC)
Molecular Weight:	655.44

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Technical Data
Citations (4) / Reviews (1)

Biological Activity for J 113863

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 for J 113863

M. Wt	655.44
Formula	C₃₀H₃₇Cl₂IN₂O₂
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	202796-41-6
PubChem ID	6918496
InChi Key	FOAFBMYSXIGAOX-LQGGPMKRSA-N
Smiles	ClC1=CC=C(OC(C=CC(Cl)=C3)=C3C2C(N[C@@H]4CC[N@@+](C/C5=C/CCCCCC5)(CC)CC4)=O)C2=C1.ClC6=CC=C(OC(C=CC(Cl)=C8)=C8C7C(N[C@H]9CC[N@+](C/C%10=C/CCCCCC%10)(CC)CC9)=O)C7=C6.[I-].[I-]

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.

Solubility for J 113863

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	65.54	100
	ethanol	32.77	50

Preparing Stock Solutions for J 113863

The following data is based on the product molecular weight 655.44.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.53 mL	7.63 mL	15.26 mL
5 mM	0.31 mL	1.53 mL	3.05 mL
10 mM	0.15 mL	0.76 mL	1.53 mL
50 mM	0.03 mL	0.15 mL	0.31 mL

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References for J 113863

References are publications that support the biological activity of the product.

Amat Pharmacological blockade of CCR1 ameliorates murine arthritis and alters cytokine networks in vivo. Br.J.Pharmacol. 2006 PMID: 17016504
Naya Design, synthesis, and discovery of a novel CCR1 antagonist. J.Med.Chem. 2001 PMID: 11311066

Citations for J 113863 (4)

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Citations are publications that use Bio-Techne products. Selected citations for J 113863 include:

Ansari et al. (2022) CCR1 antagonist J-113863 corrects the imbalance of pro- and anti-inflammatory cytokines in a SJL/J mouse model of relapsing-remitting multiple sclerosis. Immunobiology. 227:152245
PMID: 35868215
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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Effective in blocking mouse CCL6 chemotaxis in vitro

Name: Anonymous

Species: Mouse

Assay Type: In Vitro

Cell Line/Tissue: Splenic Cells

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.

As best we can tell, J113863 is entirely insoluble in water containing media. The drug was first dissolved in DMSO, and PBS added to bring to 5% DMSO. As soon as the PBS is added, the drug comes out of solution, however it has proven to still be effective in vitro at concentrations of approximately 1ug/ml and 10ug/ml

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