JTV-519 hemifumarate

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 Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. 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

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