Biological Activity
Potent chemokine CCR2b receptor antagonist (IC50 = 180 nM). Potently inhibits cell chemotaxis induced by MCP-1 (EC50 = 24 nM).
Compound Libraries
Teijin compound 1 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 476.32 |
| Formula | C21H21ClF3N3O2.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1313730-14-1 |
| PubChem ID | 56972239 |
| InChI Key | PGUQBBISBKGQDC-GMUIIQOCSA-N |
| Smiles | O=C(CNC(C3=CC=CC(C(F)(F)F)=C3)=O)N[C@@H]1CCN(CC2=CC=C(Cl)C=C2)C1.Cl |
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 | 47.63 | 100 | |
| water | 4.76 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 476.32. 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 | 2.1 mL | 10.5 mL | 20.99 mL |
| 5 mM | 0.42 mL | 2.1 mL | 4.2 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.1 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hall et al (2009) Elucidation of binding sites of dual antagonists in the human chemokine receptors CCR2 and CCR5. Mol.Pharmacol. 75 1325 PMID: 19297521
Moree et al (2004) Small molecule antagonists of the CCR2b receptor. Part 2: discovery process and initial structure-activity relationships of diamine derivatives. Bioorg.Med.Chem.Letts. 14 5413 PMID:
Moree et al (2008) Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series. Bioorg.Med.Chem.Letts. 18 1869 PMID:
Keywords: Teijin compound 1, supplier, Potent, CCR2b, antagonists, chemokines, receptors, Teijin, compound1, Chemokine, CC, Receptors, Chemokine, CC, Receptors, Tocris Bioscience
