132836-42-1
中文名稱
1,2,3,4-四氫-1-(1-萘基甲基)-6,7-異喹啉二醇?xì)滗逅猁}
英文名稱
YS 49
CAS
132836-42-1
分子式
C20H20BrNO2
分子量
386.282
MOL 文件
132836-42-1.mol
更新日期
2024/12/03 15:40:38
132836-42-1 結(jié)構(gòu)式
基本信息
中文別名
1,2,3,4-四氫-1-(1-萘基甲基)-6,7-異喹啉二醇?xì)滗逅猁} 英文別名
YS 49CS-884
YS 49
YS49
1,2,3,4-Tetrahydro-1-(1-naphthalenylmethyl)-6,7-isoquinolinediol hydrobromide
1,2,3,4-Tetrahydro-1-(1-naphthalenylmethyl)-6,7-Isoquinolinediol hydrobromide monohydrate
所屬類別
生物化工：激動(dòng)劑抑制劑
常見問題列表
生物活性
YS-49 是 PI3K/Akt (RhoA 的下游靶標(biāo)) 的激活劑，可減少 3-甲基膽堿處理的細(xì)胞中 RhoA/PTEN 的激活。YS-49 能通過誘導(dǎo)血紅素加氧酶 (HO-1) 來抑制血管緊張素 II (Ang II) 刺激 VSMC 細(xì)胞的增殖。YS-49 是異喹啉化合物生物堿，因能激活心臟 β-adrenoceptors 而具有強(qiáng)烈的正性肌力作用。體外研究
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. |
體內(nèi)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. |