Biological Activity
Extremely selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). Inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischemia-reperfusion injury in kidneys.
Technical Data
| M. Wt | 417.5 |
| Formula | C25H27N3O3 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 300816-15-3 |
| PubChem ID | 9953769 |
| InChI Key | ODNICNWASXKNNQ-UHFFFAOYSA-N |
| Smiles | CC1=C(CCN2CCC3(CC2)OC(=O)NC2=C3C=C(C)C=C2)N=C(O1)C1=CC=CC=C1 |
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 | 4.17 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 417.5. 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 | 2.4 mL | 11.98 mL | 23.95 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.79 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.4 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Mirzadegan et al (2000) Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists. J.Biol.Chem. 275 25562 PMID: 10770925
Furuichi et al (2003) CCR2 signaling contributes to ischemia-reperfusion injury in kidney. J.Am.Soc.Nephrol. 14 2503 PMID: 14514728
Kitagawa et al (2004) Blockade of CCR2 ameliorates progressive fibrosis in kidney. Am.J.Pathol. 165 237 PMID: 15215179
Keywords: RS 504393, supplier, selective, CCR2, chemokine, receptor, antagonists, CXCR, Chemokine, Receptors, RS504393, Chemokine, CC, Receptors, Chemokine, CC, Receptors, Tocris Bioscience
