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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 |
| Related CCR Products |
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| Maraviroc
Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties. |
| Vicriviroc Malate
Vicriviroc (SCH 417690) is a pyrimidine CCR5 entry inhibitor of HIV-1 with IC50 of 0.91 nM. |
| Bindarit
Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8. Bindarit also has anti-inflammatory activity. |
| BMS-813160
BMS-813160 is the first dual CCR2/CCR5 antagonist. BMS-813160 binds with CCR2, CCR5, CCR1, CCR4 and CXCR2 with IC50s of 6.2 nM, 3.6 nM, ＞25 μM, ＞40 μM and ＞40 μM, respectively. |
| INCB3284 dimesylate
INCB 3284 dimesylate is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM. |
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