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JTV-519

CAS No. 145903-06-6

JTV-519( K201 | JTV519 )

Catalog No. M11979 CAS No. 145903-06-6

JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    JTV-519
  • Note
    Research use only, not for human use.
  • Brief Description
    JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs).
  • Description
    JTV-519 (K201) is a Ca2+-dependent blocker of SERCA and a partial agonist of ryanodine receptors (RyRs); displays Ca(2+)-dependent inhibition of SERCA-dependent ATPase activity with IC50 of 9 uM at 0.25 Ca2+ in cardiac muscle; may prevent abnormal Ca(2+) leak from the sarcoplasmic reticulum (SR) in the ischemic heart and skeletal muscle (SkM) by stabilizing the ryanodine receptors (RyRs; RyR1 and RyR2, respectively).Heart Arrhythmia Phase 2 Discontinued.
  • In Vitro
    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.
  • In Vivo
    JTV-519 (0.5mg/kg/h, i.v., 2 h before the surgery) improves cardiac function in CLP mice, where thefractional shortening (FS) and ejection fraction (EF)are significantly increased as compared with CLP mice without JTV-519 treatment. 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.
  • Synonyms
    K201 | JTV519
  • Pathway
    GPCR/G Protein
  • Target
    Calcium Channel
  • Recptor
    Calcium Channel
  • Research Area
    Cardiovascular Disease
  • Indication
    Heart Arrhythmia

Chemical Information

  • CAS Number
    145903-06-6
  • Formula Weight
    424.603
  • Molecular Formula
    C25H32N2O2S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    COC1=CC2=C(C=C1)SCCN(C2)C(=O)CCN3CCC(CC3)CC4=CC=CC=C4
  • Chemical Name
    1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Darcy YL, et al. Mol Pharmacol. 2016 Aug;90(2):106-15. 2. Inagaki K, et al. Circulation. 2000 Feb 22;101(7):797-804. 3. Ito K, et al. Br J Pharmacol. 2000 Jun;130(4):767-76. 4. Nakaya H, et al. Br J Pharmacol. 2000 Dec;131(7):1363-72.
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