JTV-519 hemifumarate (K201 hemifumarate) is a Ca-dependent blocker of sarcoplasmic reticulum Ca-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
性状
Solid
体外研究(In Vitro)
JTV-519 (K201) inhibits inward Ca 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, 3 μM JTV-519 shows significant inhibition of Ca movement due to annexin V, and 50% inhibition is achieved at 25 μM K201. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Darcy YL, et al. K201 (JTV519) is a Ca-Dependent Blocker of SERCA and a Partial Agonist of Ryanodine Receptors in Striated Muscle. Mol Pharmacol. 2016 Aug;90(2):106-15.[2]. Kaneko N, et al. Inhibition of annexin V-dependent Ca2+ movement in large unilamellar vesicles by K201, a new 1,4-benzothiazepine derivative. Biochim Biophys Acta. 1997 Nov 13;1330(1):1-7.