产品
编 号:F181642
分子式:C15H8F6N2O2
分子量:362.23
产品类型
结构图
CAS No: 153587-01-0
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产品详情
生物活性:
NS-1619 is an opener of large conductance Ca2+-activated K+ (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10?–?30?μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.
体内研究:
Opening of KCa channels with NS-1619 (1 mg/kg; i.p.) can delay protection in mouse hearts.Animal Model:Adult male outbred ICR mice
Dosage:1 mg/kg
Administration:Pretreated i.p. 24 h before I/R
Result:Pretreatment induced delayed protection 24 h later.Resulted in significant cardioprotection 24 h later, i.e., infarct size was reduced from 38.8 ± 3.7% to 19.8 ± 2.9%.
体外研究:
NS1619 (5, 10, 30, 50, and 100 μM) inhibits the proliferation of A2780 cells in a dosage and time dependent manner IC50=31.1 μM for 48 h pretreatment.NS1619 (30 μM) exhibits augmenting effect on whole cell IK in human ovarian cancer cells A2780.NS1619 (10, 30, 50, and 100 μM) increases levels of p53, p21Cip1 and Bax proteins in A2780 cells.DNA content of A2780 cells was significantly decreased after 36 and 48 h of pretreatment. The breakdown of DNA results in death of the tumor cells.