JTV-519 free base  (Synonyms: K201 free base)

JTV-519 free base (K201 free base) 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) inhibits inward Ca²⁺ 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 Ca²⁺, 3 μM JTV-519 shows significant inhibition of Ca²⁺ movement due to annexin V, and 50% inhibition is achieved at 25 μM K201^[2].

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

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^[3].

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

424.60

C₂₅H₃₂N₂O₂S

145903-06-6

固体

Light yellow to yellow

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]