1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐

生物活性体外研究体内研究 1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐试剂级价格

CAS号:132836-42-1
英文名:YS 49
中文名:1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐
CBNumber:CB41390234
分子式:C20H20BrNO2
分子量:386.2823
MOL File:132836-42-1.mol

1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐化学性质

储存条件 :2-8°C
溶解度 :H2O: >10mg/mL
形态 :solid
颜色 :White to off-white

安全信息

危险品标志 :Xn,N
危险类别码 :22-50
安全说明 :61
危险品运输编号 :UN 3077 9 / PGIII
WGK Germany :3

1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐性质、用途与生产工艺

生物活性 YS-49 是 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。YS-49 能通过诱导血红素加氧酶 (HO-1) 来抑制血管紧张素 II (Ang II) 刺激 VSMC 细胞的增殖。YS-49 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。

体外研究

YS-49 (1-100 μM; 18 hours; RAVSMC and RAW 264.7 cells) concentration-dependently inhibits the accumulation of nitrite in both RAVSMC and RAW 264.7 exposed to lipopolysaccharide (LPS) plus INF-γ, with IC ₅₀ values of 22 μM and 30 μM, respectively.
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 at the transcriptional level.

Cell Viability Assay

Cell Line:	RAVSMC and RAW 264.7 cells
Concentration:	10 μΜ, 30 μΜ and 100 μΜ (RAVSMC cells); 1 μΜ, 10 μΜ and 100 μM (RAW 264.7 cells)
Incubation Time:	18 hours
Result:	Inhibited the accumulation of nitrite in both RAVSMC and RAW 264.7 exposed to LPS+INF-γ, with IC ₅₀ values of 22 and 30 μM, respectively.

Western Blot Analysis

Cell Line:	RAVSMC and RAW 264.7 cells
Concentration:	10 μΜ, 30 μΜ and 100 μΜ
Incubation Time:	18 hours
Result:	Concentration-dependently inhibited the expression of iNOS protein induced by LPS plus IFN-γ.

体内研究

YS-49 (5 mg/kg; intraperitoneal injection; 8 hours; male Sprague Dawley rats) treatment significantly reduces serum NOx levels in LPS-treated rats, the NOx levels reduce from 86 μM to 34 μM.

Animal Model:	Male Sprague Dawley rats (250-300 g)
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; 8 hours
Result:	Serum NOx levels were significantly reduced.