Biological Activity
Potent, selective hCCR2 antagonist. Exhibits potent antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity (IC50 values are 3.7 and 4.7 nM respectively). Also displays weak hERG activity; inhibits the hERG potassium current (IC50 = 84μM). Orally bioavailable.
Technical Data
| M. Wt | 712.76 |
| Formula | C26H31F3N4O4.2CH4O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 887401-93-6 |
| PubChem ID | 11679268 |
| InChI Key | PNPNUHKICDECDH-SEBNIYPMSA-N |
| Smiles | O=C(NCC(N[C@@H]2CCN([C@H]3CC[C@](C4=CC=C(OC)N=C4)(O)CC3)C2)=O)C1=CC(C(F)(F)F)=CC=C1.CS(=O)(O)=O.CS(=O)(O)=O |
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 | 71.28 | 100 | |
| water | 71.28 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 712.76. 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 | 1.4 mL | 7.01 mL | 14.03 mL |
| 5 mM | 0.28 mL | 1.4 mL | 2.81 mL |
| 10 mM | 0.14 mL | 0.7 mL | 1.4 mL |
| 50 mM | 0.03 mL | 0.14 mL | 0.28 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Xue et al (2011) Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist. ACS.Med.Chem.Lett. 2 450 PMID:
Keywords: INCB 3284 dimesylate, supplier, INCB3284, CCR2, antagonist, antagonists, hCCR2, human, chemokine, receptor, receptors, Chemokine, CC, Receptors, Chemokine, CC, Receptors, Tocris Bioscience
