| Bioactivity | TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency[1]. |
| Invitro | TGF-β1/Smad3-IN-1 (100-500 nM; 48 h) 导致 H2228 细胞的 TGF-β1 水平降低,比相同浓度的 nintedanib 现出更好的抑制作用[1]。TGF-β1/Smad3-IN-1 (2-6 μM; 24 h) 表现出剂量依赖性抑制 p-Smad3 和 α-SMA 表达,显著抑制 NIH3T3 细胞迁移[1]。TGF-β1/Smad3-IN-1 (3-10 μM; 72 h) 增加 NIH3T3 细胞中的 Cleave-casepase3 的表达,剂量依赖性的诱导细胞凋亡[1]。TGF-β1/Smad3-IN-1 对于 NIH3T3 细胞的 IC50 为 1.07 μM。对于 TGFβ1 激活的 HFL1 细胞的 IC50 为 2.86 ± 0.014 μM。有效地抑制了活化标志物 α-SMA 的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> TGF-β1/Smad3-IN-1 相关抗体: Apoptosis Analysis[1] Cell Line: |
| In Vivo | TGF-β1/Smad3-IN-1 在 SD 大鼠中的生物利用度高于 Nintedanib (HY-50904)[1]。TGF-β1/Smad3-IN-1 (p.o.; 100 mg/kg/; 第二到二十天) 处理博来霉素诱导的小鼠肺纤维化模型，可以抑制博莱霉素诱导的肺 TGFβ1和 HYP 的表达，减少细胞外间质沉积，减轻肺纤维化[1]。药代动力学分析[1] Route |
| Formula | C30H34N4O6S |
| Molar Mass | 578.68 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. An B, et al. Inhibition of TGF-β1/Smad3 signaling by compound 5aa: A potential treatment for idiopathic pulmonary fibrosis. Bioorg Chem. 2024 Apr 16;147:107374. |