J 113863

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Cat.No. 2595 - J 113863 | C30H37Cl2IN2O2 | CAS No. 353791-85-2
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)
Datasheet
Citations (3)
Literature

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 353791-85-2
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 655.44. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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


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

3 Citations for J 113863

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

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

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


Do you know of a great paper that uses J 113863 from Tocris? If so please let us know.

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