Vesnarinone

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

Vesnarinone (INN) 是一种混合磷酸二酯酶 3 抑制剂和离子通道调节剂，具有适度的、剂量依赖性的正性肌力活性。

Vesnarinone is a cardiotonic agent, mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. Vesnarinone improves ventricular performance most in patients with the worst degree of heart failure.(In Vitro):Vesnarinone (60 and 100 μg/mL; 48 h) inhibits the cell growth in a dose-dependent manner.Vesnarinone (60 μg/mL; 48 h) induces G1 arrest and apoptosis.Vesnarinone (60 μg/mL; 0, 12, 24, and 48 h) treatment increases p21-mRNA expression and decreases p21 protein slightly.(In Vivo):Vesnarinone (oral gavage; 300 mg/kg; once daily; 6 w) binds covalently to rat liver in vivo.

Vesnarinone (60 and 100 μg/mL; 48 h) inhibits the cell growth in a dose-dependent manner.Vesnarinone (60 μg/mL; 48 h) induces G1 arrest and apoptosis.Vesnarinone (60 μg/mL; 0, 12, 24, and 48 h) treatment increases p21-mRNA expression and decreases p21 protein slightly. Cell Viability AssayCell Line:OSC3, OSC4, and OSC5 cells Concentration:60 μg/mL and 100 μg/mL Incubation Time:48 hours Result:Observed more than 50% inhibition in cells treated with 100 μg/mL, and reduced 30±40% the production of MTT formazan in cells treated with 60 μg/mL.Apoptosis Analysis Cell Line:OSC3, OSC4, and OSC5 cells Concentration:60 μg/mL Incubation Time:48 hours Result:Decreased the tumor cell population in the S phase and increased in the G1 phase.Western Blot Analysis Cell Line:OSC3, OSC4, and OSC5 cells Concentration:60 μg/mL Incubation Time:0, 12, 24, and 48 hours Result:Increased the expression of p21-mRNA after 12±24 h vesnarinone treatment.

Vesnarinone (oral gavage; 300 mg/kg; once daily; 6 w) binds covalently to rat liver in vivo. Animal Model:Female Lewis rats (200 g)Dosage:300 mg/kg Administration:Oral gavage; 300 mg/kg; once daily; 6 weeks Result:Observed covalently modified liver proteins.

RG-0210 | RG 0210 | Piteranometozine | Vesnarinone

PI3K/Akt/mTOR signaling

GSK-3

Others

Infection

——

81840-15-5

395.46

C22H25N3O4

>98% (HPLC)

DMSO : 16.67 mg/mL. 42.15 mM;

N1C(=O)CCc2cc(ccc12)N1CCN(CC1)C(=O)c1cc(c(cc1)OC)OC

6-[4-(3,4-dimethoxybenzoyl)piperazin-1-yl]-3,4-dihydro-1H-quinolin-2-one

(-20℃)

With Ice Pack

≥ 2 years