YS-49 是一种PI3K/Akt(RhoA 的下游靶标) 的激活剂,可减少 3-甲基胆碱处理的细胞中 RhoA/PTEN 的激活。它是异喹啉化合物生物碱,因能激活心脏β-adrenoceptors而具有强烈的正性肌力作用。它能通过诱导血红素加氧酶来抑制血管紧张素 II 刺激 VSMC 细胞的增殖。
产品描述
YS-49 is an activator of PI3K/Akt (a downstream target of RhoA).
体外活性
In RAVSMC and RAW 264.7 cells, YS-49 (1-100?μM; 18 hours; ) concentration-dependently inhibits the accumulation of nitrite in both RAVSMC and RAW 264.7 exposed to lipopolysaccharide (LPS) plus INF-γ, with IC50 values of 22 μM and 30?μM, respectively[2].At the transcriptional level, YS-49 (10-100?μM; 18 hours; RAVSMC and RAW 264.7 cells) suppresses iNOS gene expression induced by LPS and/or cytokines in RAVSMC and RAW 264.7 cells [2].
体内活性
In male Sprague Dawley rats,YS-49 (5?mg/kg; intraperitoneal injection; 8 hours) treatment significantly reduces serum NOx levels in LPS-treated rats, the NOx levels reduce from 86 μM to 34 μM[2].
Cas No.
132836-42-1
分子式
C20H20BrNO2
分子量
386.28
储存和溶解度
H2O:10 mg/mL (25.89 mM),ultrasonic and warming and heat to 60°C
DMSO:100 mg/mL (258.88 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years