JTV-519 hemifumarate (Synonyms: K201 hemifumarate)
目录号: PL04400 纯度: ≥98%
CAS No. :1435938-25-2
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中文名称
JTV-519 hemifumarate
英文名称
JTV-519 hemifumarate
英文别名
JTV-519 hemifumarate
Cas No.
1435938-25-2
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
JTV-519 hemifumarate (K201 hemifumarate) 是 Ca2+ 依赖性的肌质网 Ca2+ 刺激的 ATP 酶 (SERCA) 阻断剂。JTV-519 hemifumarate (K201 hemifumarate) 也是横纹肌中兰尼碱受体 (ryanodine receptors) 的部分激动剂。JTV-519 hemifumarate (K201 hemifumarate) 是一种心脏保护剂,具有抗心律失常作用。
生物活性
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.
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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