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INCB3284 is a potent, selective, and orally bioavailable hCCR2 antagonist, exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2. INCB3284 exhibited an IC50 of 4.7 nM in antagonism of chemotaxis activity, an IC50 of 84 μM in inhibition of the hERG potassium current, a free fraction of 58% in protein binding, high selectivity over other chemokine receptors and G-protein-coupled receptors, and acceptable oral bioavailability in rodents and primates.
Molecular Weight | 520.54 |
Formula | C26H31F3N4O4 |
CAS Number | 887401-92-5 |
Solubility (25°C) | DMSO ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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