1435938-25-2
中文名称
JTV-519 HEMIFUMARATE
英文名称
JTV-519 hemifumarate
CAS
1435938-25-2
分子式
C29H36N2O6S
分子量
540.68
MOL 文件
1435938-25-2.mol
1435938-25-2 结构式
常见问题列表
生物活性
JTV-519 hemifumarate (K201 hemifumarate) 是 Ca2+ 依赖性的肌质网 Ca2+ 刺激的 ATP 酶 (SERCA) 阻断剂。JTV-519 hemifumarate (K201 hemifumarate) 也是横纹肌中兰尼碱受体 (ryanodine receptors) 的部分激动剂。JTV-519 hemifumarate (K201 hemifumarate) 是一种心脏保护剂，具有抗心律失常作用。体外研究
JTV-519 (K201) inhibits inward Ca 2+ movement into large unilamellar vesicles (LUV) caused by annexin V in a dose-dependent manner. In the presence of 50 nM annexin V and 400 μM Ca 2+ , 3 μM JTV-519 shows significant inhibition of Ca 2+ movement due to annexin V, and 50% inhibition is achieved at 25 μM K201.
体内研究
JTV-519 (0.5mg/kg/h, i.v., 2 h before the surgery) improves cardiac function in CLP mice, where the fractional shortening (FS) and ejection fraction (EF) are significantly increased as compared with CLP mice without JTV-519 treatment.
| Animal Model: | Wild type male C57BL/6 mice weighing 18-22g with polymicrobial sepsis produced by cecal ligation and puncture (CLP) |
| Dosage: | 0.5 mg/kg/h |
| Administration: | Applied intraperitoneally 2 h before the surgery |
| Result: | Improved cardiac function, where the EF and FS were significantly increased. |