TGFβ1-IN-3

Research use only, not for human use.

TGFβ1-IN-3, a diarylhydrazone derivative, inhibits fibroblast activation and proliferation, positioning it as a candidate compound for the treatment of idiopathic pulmonary fibrosis (IPF).

TGFβ1-IN-3 is a diarylacylhydrazones derivative that effectively suppresses the activation and proliferation of fibroblasts. TGFβ1-IN-3 can be used for idiopathic pulmonary fibrosis (IPF) research.

TGFβ1-IN-3 (compound 44) shows inhibitory effect against NIH-3T3 cells with an IC50 of 0.57 μM.TGFβ1-IN-3 (compound 44; 10 μM; for 24 h) inhibits TGF-β1-induced abnormal activation of NIH-3T3 and A549 cells, as well as migration and epithelial-mesenchymal transition (EMT) of A549 cells.TGFβ1-IN-3 (compound 44) could bind to STAT3, and able to interact with Ile659, and the hydrophilic group piperidine formed intermolecular forces with Ser636, Arg609, and Pro639. The nitrofuran of TGFβ1-IN-3 could interact with Lys658.Western Blot Analysis Cell Line:NIH-3T3 or A549 cells Concentration:10 μM Incubation Time:24 h Result:Were able to inhibit TGF-β1-induced activation of fibroblasts in vitro.

TGFβ1-IN-3 (compound 44; 30-60 mg/kg; p.o; once daily; for 22 days) improves mouse lung function and slowsthe progression of IPF. TGFβ1-IN-3 could reverse the pulmonary fibrosis in treatment model. Pharmacokinetic parameters of TGFβ1-IN-3 (compound 44) in rats.Animal Model:C57BL/6 mice (6-10 weeks) injected with Bleomycin for establishing pulmonary fibrosis model.Dosage:30 mg/kg, 60 mg/kg Administration:Orally administration; once daily; for 22 days Result:Could reverse the pulmonary fibrosis in treatment model.

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2883813-58-7

442.51

C23H30N4O5

>98% (HPLC)

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C(=N/NC(=O)C1=CC=C(OCCCCCCN2CCCCC2)C=C1)\C=3OC(N(=O)=O)=CC3

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(-20℃)

With Ice Pack

≥ 2 years