| Description | PF-05221304 (NSC-170984) is an orally active, liver-targeted inhibitor of acetyl-CoA carboxylase (ACC), a rate-limiting enzymes for fatty acid synthesis. |
| In vitro | PF-05221304 阻断了人类T细胞向促炎而非抗炎T细胞的极化，并在体外抑制了原代人类星状细胞向肌成纤维细胞的激活，直接显示出其对炎症和纤维生成的影响[1]。 |
| In vivo | PF-05221304 在二乙基亚硝胺化学诱导的肝损伤模型以及胆碱缺乏、高脂饲料喂养的大鼠模型中[1]，降低了炎症和纤维化的标志物。 |
| Synonyms | STAT5 Inhibitor III, NSC 170984, R 6238,, Clesacostat |
| molecular weight | 502.56 |
| Molecular formula | C28H30N4O5 |
| CAS | 1370448-25-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 95mg/ml(189.03mM) ethanol: 5mg/ml(9.95mM) |
| References | 1. Ross T T , Crowley C , Kelly K L , et al. Acetyl-CoA Carboxylase Inhibition Improves Multiple Dimensions of NASH Pathogenesis in Model Systems[J]. Cellular and Molecular Gastroenterology and Hepatology, 2020, 10(4). |