| Description | TGFβ1-IN-3 is a diarylhydrazone derivative with inhibitory effects on fibroblast activation and proliferation.TGFβ1-IN-3 is a candidate compound for the treatment of idiopathic pulmonary fibrosis (IPF). |
| In vitro | TGFβ1-IN-3对NIH-3T3细胞的抑制作用，IC50为0.57 μM。在10 μM浓度和24小时处理下，TGFβ1-IN-3能够抑制TGF-β1诱导的NIH-3T3和A549细胞的异常激活，以及A549细胞的迁移和上皮-间充质转化（EMT）。TGFβ1-IN-3能够与STAT3结合，并与Ile659进行相互作用，其亲水基团哌啶通过分子间力与Ser636、Arg609和Pro639形成相互作用。TGFβ1-IN-3中的硝基呋喃能够与Lys658发生相互作用。[1] |
| In vivo | TGFβ1-IN-3（30-60 mg/kg; p.o.; 每日一次; 22天; C57BL/6小鼠）能缓慢特发性肺纤维化（IPF）的进程并改善小鼠的肺功能。在治疗模型中，TGFβ1-IN-3有能力逆转肺纤维化。[1] |
| molecular weight | 442.51 |
| Molecular formula | C23H30N4O5 |
| CAS | 2883813-58-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (101.69 mM) |
| References | 1. Xingping Su, et al. Design, synthesis and biological evaluation of novel diarylacylhydrazones derivatives for the efficient treatment of idiopathic pulmonary fibrosis. Eur J Med Chem. 2023 Jan 5;245(Pt 2):114918. |