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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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| C-021 dihydrochloride
C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. |
| C-021
C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. |
| AZD-5672
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). |
| MLN3126
MLN3126 is an orally active and potent CCR9 antagonist. |
| AZD2423
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. |
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Products are for research use only. Not for human use. We do not sell to patients.
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