| Description | C-021 dihydrochloride is a potent CCR4 antagonist. It potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM. |
| In vitro | C-021有效地阻止人源CCL22衍生的[35S]GTPγS与受体结合（IC50：18 nM）。在人肝微粒体（HML）中，C-021展现出17,377 mL/h/kg[1]的内在清除率（CLint）。 |
| In vivo | 在小鼠恶唑酮诱导的接触过敏试验中，皮下注射 C-021 后药效非常明显。然而，当口服 C-021 时，几乎观察不到抑制作用[1]。C-021（1 毫克/千克；静脉注射；每天；连续 3 天）可显著减轻急性肝衰竭小鼠的微神经胶质增生[2]。 |
| molecular weight | 540.57 |
| Molecular formula | C27H43Cl2N5O2 |
| CAS | 1784252-84-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5.41 mg/mL (10 mM), Sonication is recommended. |
| References | 1. Yokoyama K, et al. Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem. 2009 Jan 1;17(1):64-73. 2. McMillin M, Frampton G, Thompson M, Galindo C, Standeford H, Whittington E, Alpini G, DeMorrow S. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10;11:121. |