JTV-519

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JTV-519 (K201) 是一种 Ca2+ 依赖性 SERCA 阻断剂和兰尼碱受体 (RyRs) 的部分激动剂。

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.

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.

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.

K201 | JTV519

GPCR/G Protein

Calcium Channel

Calcium Channel

Cardiovascular Disease

Heart Arrhythmia

145903-06-6

424.603

C25H32N2O2S

>98% (HPLC)

——

COC1=CC2=C(C=C1)SCCN(C2)C(=O)CCN3CCC(CC3)CC4=CC=CC=C4

1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone

(-20℃)

With Ice Pack

≥ 2 years