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Submit ReviewJ 113863
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)
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 Data 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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Product Datasheets for J 113863
References for J 113863
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for J 113863, please let us know.
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Keywords: J 113863, J 113863 supplier, Potent, CCR1, chemokine, receptor, antagonists, CXCR, Receptors, J113863, Rantes, Chemokine, CC, 2595, Tocris Bioscience
4 Citations for J 113863
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
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
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
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? Please let us know.
Reviews for J 113863
Average Rating: 5 (Based on 1 Review.)
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Effective in blocking mouse CCL6 chemotaxis in vitro.
By
Anonymous on 12/12/2017
Assay Type: In Vitro
Species: Mouse
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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