JTV-519 hemifumarate (C09-1140-861)

JTV-519 hemifumarate (K201 hemifumarate) is a Ca 2+ -dependent blocker of sarcoplasmic reticulum Ca 2+ -stimulated ATPase ( SERCA ) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.In VitroJTV-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoJTV-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.Form:Solid. Specification: 0.98 Molecular Formula: C25H32N2O2S.1/2C4H4O4 Molecular Weight: 482.64