1435938-25-2
中文名稱
JTV-519 HEMIFUMARATE
英文名稱
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 結(jié)構(gòu)式
常見問題列表
生物活性
JTV-519 hemifumarate (K201 hemifumarate) 是 Ca2+ 依賴性的肌質(zhì)網(wǎng) Ca2+ 刺激的 ATP 酶 (SERCA) 阻斷劑。JTV-519 hemifumarate (K201 hemifumarate) 也是橫紋肌中蘭尼堿受體 (ryanodine receptors) 的部分激動(dòng)劑。JTV-519 hemifumarate (K201 hemifumarate) 是一種心臟保護(hù)劑，具有抗心律失常作用。體外研究
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.
體內(nèi)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. |