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CAS No. : 101975-10-4
MCE 国际站:Zardaverine
产品活性:Zardaverine是一种口服有效的和具有选择性的 PDE3/4 抑制剂 (IC50)=0.58 uM/0.17 uM),具有强大的支气管扩张活性。Zardaverine 还可选择性地抑制 HCC 细胞增殖,并诱导细胞凋亡和周期停滞 (G0/G1 期)。Zardaverine 具有较好的抗肿瘤潜力,并且在哮喘中的支气管松弛和减少炎症方面均有效。
研究领域:Metabolic Enzyme/Protease | Apoptosis
作用靶点:Phosphodiesterase (PDE) | Apoptosis
In Vitro: Zardaverine (0-30 µM; 72 h) selectively inhibits the growth of human HCC cells in vitro.
Zardaverine shows selective antitumor activity that closely related to the regulation of cell cycle-associated proteins, but is independent of PDE3/4 inhibition.
Zardaverine (0.1 µM; 24 h) selectively causes G0/G1-phase arrest and dysregulates cell cycle-associated proteins in HCC cells.
Zardaverine (0.01, 0.03, 0.1, 0.3 1 µM/48h; 0.3 1 µM/24, 36, 48, 60, 72 h) induces apoptosis in a time- and concentration- dependent manner, in Bel-7402 and SMMC-7721 cells.
In Vivo: Zardaverine (60, 200 mg/kg; p.o.; single daily for 14 days) inhibits the growth of human Bel-7402 xenografts in mice.
Zardaverine (8046.6 µg/kg; i.p.; single) blocks the LPS induced increase in responsiveness completely in airway inflammation and hyperresponsiveness rat model.
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