1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐
| 中文名称 | 1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐 |
|---|---|
| 中文同义词 | 1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐;化合物YS-49;1-(萘-1-基甲基)-1,2,3,4-四氢异喹啉-6,7-二醇氢溴酸盐 |
| 英文名称 | YS 49 |
| 英文同义词 | YS 49;1,2,3,4-Tetrahydro-1-(1-naphthalenylmethyl)-6,7-Isoquinolinediol hydrobromide monohydrate;1,2,3,4-Tetrahydro-1-(1-naphthalenylmethyl)-6,7-isoquinolinediol hydrobromide;CS-884;YS 49;YS49;inhibit,YS-49,PI3K,Adrenergic Receptor,Phosphoinositide 3-kinase,PKB,Beta Receptor,YS 49,Akt,Protein kinase B,Inhibitor,YS49,Angiotensin Receptor |
| CAS号 | 132836-42-1 |
| 分子式 | C20H20BrNO2 |
| 分子量 | 386.2823 |
| EINECS号 | |
| 相关类别 | Akt;mTOR;PI3K;PI3K/Akt/mTOR |
| Mol文件 | 132836-42-1.mol |
| 结构式 |  |
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
| 储存条件 | 2-8°C |
|---|---|
| 溶解度 | H2O：>10mg/mL |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
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。
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. |
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. |