JTV-519  (Synonyms: K201)

JTV-519 (K201) 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^[1][2].

JTV-519 (K201) 以剂量依赖的方式抑制由膜联蛋白 V 引起的 Ca²⁺ 向内移动到大单层囊泡 (LUV)。在 50 nM 膜联蛋白 V 和 400 μM Ca²⁺ 存在的情况下，3 μM JTV-519 对 Ca²⁺ 的抑制作用显著，25 μM K201 的抑制作用达到 50%^[2]。

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

JTV-519 (0.5mg/kg/h，术前 2 h 静脉注射) 可改善 CLP 小鼠的心功能，其中与未经 JTV-519 处理的 CLP 小鼠相比，分数缩短 (FS) 和射血分数 (EF) 显著增加^[3]。

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

461.06

C₂₅H₃₃ClN₂O₂S

1038410-88-6

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Darcy YL, et al. K201 (JTV519) is a Ca²⁺-Dependent Blocker of SERCA and a Partial Agonist of Ryanodine Receptors in Striated Muscle. Mol Pharmacol. 2016 Aug;90(2):106-15.  [Content Brief]

  [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.  [Content Brief]

  [3]. Yang J, et al. Toll-like receptor 4-induced ryanodine receptor 2 oxidation and sarcoplasmic reticulum Ca²⁺ leakage promote cardiac contractile dysfunction in sepsis. J Biol Chem. 2018 Jan 19;293(3):794-807.  [Content Brief]