产品
编 号：F010134
分子式：C12H10F2N2O3
分子量：268.22
分子式：C12H10F2N2O3
分子量：268.22
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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结构图
CAS No: 101975-10-4
产品详情
生物活性：
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma.
体内研究：
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.Animal Model:Female Balb/cA-nude mice (5 to 6-week-old; human Bel-7402 xenografts model).
Dosage:60, 200 mg/kg
Administration:Oral administration; single daily for 14 days
Result:Inhibited the growth of Bel-7402 xenografts at the dose of 60 mg/kg for 14 consecutive days and caused the tumor regression at the dose of 200 mg/kg.
Animal Model:Inbred male Fisher 344 (F344) rats (250-350 g; 3 to 4-month-old; airway inflammation and hyperresponsiveness model).
Dosage:8046.6 μg/kg (30 μmol/Kg)
Administration:Intraperitoneal injection; single
Result:Completely blocked LPS-induced hyperresponsiveness and airway inflammation.
体外研究：
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.
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma.
体内研究：
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.Animal Model:Female Balb/cA-nude mice (5 to 6-week-old; human Bel-7402 xenografts model).
Dosage:60, 200 mg/kg
Administration:Oral administration; single daily for 14 days
Result:Inhibited the growth of Bel-7402 xenografts at the dose of 60 mg/kg for 14 consecutive days and caused the tumor regression at the dose of 200 mg/kg.
Animal Model:Inbred male Fisher 344 (F344) rats (250-350 g; 3 to 4-month-old; airway inflammation and hyperresponsiveness model).
Dosage:8046.6 μg/kg (30 μmol/Kg)
Administration:Intraperitoneal injection; single
Result:Completely blocked LPS-induced hyperresponsiveness and airway inflammation.
体外研究：
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.
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