| Identification | Back Directory | [Name]
Benzamide, N-cyclopentyl-3-[[3-(4-methoxyphenyl)-1-oxo-2-propen-1-yl]amino]- | [CAS]
2348795-14-0 | [Synonyms]
Benzamide, N-cyclopentyl-3-[[3-(4-methoxyphenyl)-1-oxo-2-propen-1-yl]amino]- | [Molecular Formula]
C22H24N2O3 | [MOL File]
2348795-14-0.mol | [Molecular Weight]
364.44 |
| Chemical Properties | Back Directory | [Boiling point ]
636.1±55.0 °C(Predicted) | [density ]
1.20±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
13.47±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
TGFβ1-IN-1 (compound 42) is a potent, orally active TGF-β1 inhibitor. TGFβ1-IN-1 inhibits the upregulation of TGF-β1-induced fibrosis markers (α-SMA and fibronectin) and can be used in liver fibrosis disease studies[1]. | [in vivo]
TGFβ1-IN-1 (compound 42) (p.o., 15 or 30 mg/kg, daily, 3weeks) prevents CCl4-induced liver injury and fibrosis, inhibits the activation of hepatic stellate cell (HSC) and epithelial-mesenchymal transition (EMT), and improves the immune microenvironment of CCl4-induced liver fibrosis as well as CCl4-induced systemic toxicity in C57BL/6J mice[1].
| Animal Model: | Liver fibrosis C57BL/6J mice induced by CCl4[1] | | Dosage: | 15 or 30 mg/kg | | Administration: | Oral administration; daily; 3 weeks | | Result: | Significantly prevented CCl4-induced liver injury and reduced liver weight factor, serum ALT, AST, CHO and TG levels.
Significantly improved structural damage and inflammatory cell infiltration in the liver, and reduced collagen deposition in liver tissue.
Reduced accumulation of CCl4-induced immune cells, such as hepatic macrophages (F4/80+ CD11b+), Th1 cells (CD69+ CD4+), and Th2 cells (CD69+ CD8+) so on.
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| [References]
[1] Lin Yue, et al. Discovery and evaluation of phenacrylanilide derivatives as novel potential anti-liver fibrosis agents. Eur J Med Chem. 2022 Nov 15;242:114685. DOI:10.1016/j.ejmech.2022.114685 |
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