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