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JTV-519
CAS No. 145903-06-6
JTV-519 ( K201 | JTV519 )
产品货号. M11979 CAS No. 145903-06-6
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。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 25MG | ￥9858 | 有现货 |
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| 50MG | ￥12834 | 有现货 |
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| 100MG | ￥15750 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称JTV-519
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注意事项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
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产品简述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。
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产品描述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.
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体外实验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.
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体内实验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.
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同义词K201 | JTV519
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通路GPCR/G Protein
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靶点Calcium Channel
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受体Calcium Channel
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研究领域Cardiovascular Disease
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适应症Heart Arrhythmia
化学信息
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CAS Number145903-06-6
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分子量424.603
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分子式C25H32N2O2S
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纯度>98% (HPLC)
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溶解度——
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SMILESCOC1=CC2=C(C=C1)SCCN(C2)C(=O)CCN3CCC(CC3)CC4=CC=CC=C4
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化学全称1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
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.
