Biological Activity
Potent, noncompetitive human CCR2 antagonist; inhibits MCP-1-induced Ca2+ mobilization in hCCR2-CHO cells (IC50 = 13 nM). Exhibits selectivity for CCR2 over CCR1, CCR3-8 and CXCR1-3. Delays onset and reduces neurological signs in an experimental autoimmune encephalomyelitis model of multiple sclerosis in hCCR2 knock-in mice. Orally active.
Compound Libraries
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Technical Data
| M. Wt | 379.38 |
| Formula | C17H15F2N3O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 871313-59-6 |
| PubChem ID | 11703589 |
| InChI Key | SYARXICKXVXWNA-LBPRGKRZSA-N |
| Smiles | FC1=CC([C@H](CC)N2C(C(OC)=O)=C(C3=CC=NO3)NC2=S)=CC=C1F |
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 | 37.94 | 100 | |
| ethanol | 37.94 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 379.38. 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 | 2.64 mL | 13.18 mL | 26.36 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.27 mL |
| 10 mM | 0.26 mL | 1.32 mL | 2.64 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Buntinx et al (2008) Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor J.Pharmacol.Exp.Ther. 327 1 PMID: 18599682
Keywords: JNJ 27141491, supplier, JNJ27141491, Chemokine, CC, Receptors, Chemokine, CC, Receptors, Tocris Bioscience
