Zardaverine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

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.

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.Cell Proliferation Assay Cell Line:Bel-7402, Bel-7404, QGY-7701 and SMMC-7721 Concentration:0-30 μM Incubation Time:72 h Result:Selectively inhibited SMMC-7721, QGY-7701, Bel-7402 and Bel-7404 growth with IC50s of 36.6, 51.0, 137.7 and 288.0, respectively.Cell Cycle Analysis Cell Line:Bel-7402, Bel-7404, QGY-7701 and SMMC-7721 Concentration:0.1 μM Incubation Time:24 h Result:Induced accumulation of Bel-7402, Bel-7404, QGY-7701 and SMMC-7721 cells in the G0/G1 phase.Western Blot Analysis Cell Line:Bel-7402, SMMC-7721 Concentration:0.01, 0.03, 0.1, 0.3 1 μM; 0.3 1 μM Incubation Time:48 h; 24, 36, 48, 60, 72 h Result:Induced a concentration- and time- dependent increase in the cleavage of PARP and caspase-3, -8 and -9, which are apoptosis markers.

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 hyper responsiveness model).Dosage:8046.6 μg/kg (30 μmol/Kg) Administration:Intraperitoneal injection; single Result:Completely blocked LPS-induced hyper responsiveness and airway inflammation.

——

Angiogenesis

PDE

PDE

——

——

101975-10-4

268.22

C12H10F2N2O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (93.21 mM; 超声助溶 )

COc1cc(ccc1OC(F)F)-c1ccc(=O)[nH]n1

——

(-20℃)

With Ice Pack

≥ 2 years