产品
编 号：F168668
分子式：C25H32N2O2S
分子量：424.6
分子式：C25H32N2O2S
分子量：424.6
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CAS No: 145903-06-6
产品详情
生物活性：
JTV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
体内研究：
JTV-519 (0.5mg/kg/h, i.v., 2 h before the surgery) improves cardiac function in CLP mice, where thefractional 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.
体外研究：
JTV-519 (K201) inhibits inward Ca2+ 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 Ca2+, 3 μM JTV-519 shows significant inhibition of Ca2+ movement due to annexin V, and 50% inhibition is achieved at 25 μM K201.
JTV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
体内研究：
JTV-519 (0.5mg/kg/h, i.v., 2 h before the surgery) improves cardiac function in CLP mice, where thefractional 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.
体外研究：
JTV-519 (K201) inhibits inward Ca2+ 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 Ca2+, 3 μM JTV-519 shows significant inhibition of Ca2+ movement due to annexin V, and 50% inhibition is achieved at 25 μM K201.
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