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TGFβ1-IN-2

Catalog No. T75004 CAS 2700263-58-5

TGFβ1-IN-2, a derivative of diarylacylhydrazones, effectively inhibits fibroblast activation and proliferation and holds potential for idiopathic pulmonary fibrosis (IPF) research [1].

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TGFβ1-IN-2, CAS 2700263-58-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 397.00
5 mg	In stock	$ 970.00
10 mg	In stock	$ 1,180.00
25 mg	In stock	$ 1,580.00
50 mg	In stock	$ 1,980.00
100 mg	In stock	$ 2,500.00

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Purity: 99.2%

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Description	TGFβ1-IN-2, a derivative of diarylacylhydrazones, effectively inhibits fibroblast activation and proliferation and holds potential for idiopathic pulmonary fibrosis (IPF) research [1].
In vitro	TGFβ1-IN-2 (compound 52) exhibits inhibition of NIH-3T3 cells with an IC50 of 1.36 μM [1]. Additionally, at a concentration of 6 μM over 24 hours, it suppresses TGF-β1-induced overactivity in both NIH-3T3 and A549 cells and inhibits migration and epithelial-mesenchymal transition (EMT) in A549 cells [1]. TGFβ1-IN-2 (compound 52) also binds to STAT3, interacting with Ile659, while its piperidine hydrophilic group forms intermolecular forces with Ser636, Arg609, and Pro639 [1].
In vivo	TGFβ1-IN-2 (compound 52) administered orally at a dosage of 30-60 mg/kg once daily for 22 days has been shown to enhance pulmonary function and decelerate the progression of Idiopathic Pulmonary Fibrosis (IPF) in mice. Additionally, this compound can potentially reverse established pulmonary fibrosis in a treatment model [1]. In rats, the pharmacokinetic profile of TGFβ1-IN-2 includes a maximum plasma concentration (C max) of 470.58±60.67 ng/mL following intravenous administration at 2 mg/kg and 351.01±85.44 ng/mL post oral administration at 20 mg/kg. The time to reach C max (T max) was 0.08 hours for intravenous and 2.17 hours for oral administration. The area under the curve (AUC 0-∞) was 370.81±76.46 h·ng/mL intravenously and 1503.71±319.62 h·ng/mL orally. The clearance rate (CL) was 5565.86±1257.13 mL/h/kg intravenously. The half-life (T 1/2) of TGFβ1-IN-2 was 0.93±0.43 hours intravenously and 1.23±0.15 hours orally, with an oral bioavailability (F) of 42.08±8.93% [1].

Molecular Weight	458.57
Formula	C23H30N4O4S
CAS No.	2700263-58-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/ml

References and Literature

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.

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Keywords

TGFβ1-IN-2 2700263-58-5 Others inhibitor inhibit

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