产品
编 号:F197686
分子式:C22H27N2O5P
分子量:430.43
产品类型
结构图
CAS No: 164083-84-5
联系客服
产品详情
生物活性:
LY-311727 is a potent secretory non-pancreatic phospholipase A2 (sPLA2) inhibitor (IC50 <1 μM for group IIA sPLA2). sPLA2 is an important proinflammatory enzyme.
体内研究:
LY-311727 (3-30 mg/kg; i.v.) dramatically suppresses the circulating enzyme activity in mice with metallothionein promoter-human secretory PLA2 minigene (Mt-sPLA2) transgenic the intravenous (i.v.) administration.Animal Model:C57BL/6J mice, Mt-sPLA2 transgenic mice model
Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:Intravenous injection
Result:Significantly and dose dependently suppressed the PLA2 activity in the serum.
体外研究:
LY-311727 (0.1-10 μM) suppresses the contractile responses induced by human non-pancreatic secretory phospholipase A2 (hnps-PLA2), in a concentration relatedmanner.LY-311727 nearly abolishes the hnps-PLA2 responses at 1 μM, while it failed to suppress porcine pancreatic PLA2 concentration response curves at the same concentration.LY-311727 displays 1,500-fold selectivity when assayed against porcine pancreatic s-PLA2.