JTV-519 free base  ≥98%

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包装规格:5mg in glass bottle
溶解性:溶于DMSO(10mg/mL )
产品描述:基本信息 产品编号: J90001 产品名称: JTV-519 free base CAS: 145903-06-6   储存条件 粉末 2-8℃ 四年     分子式: C25H32N2O2S 溶于液体 -80℃ 6个月 分子量: 424.60 -20℃ 1个月 化学名:  3-(4-benzylpiperidin-1-yl)-1-(7-methoxy-3,5-dihydro-2H-1,4-benzothiazepin-4-yl)propan-1-one Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   生物活性 产品描述 Ca2+依赖性的肌质网Ca2+刺激的ATP酶(SERCA)阻断剂。JTV-519 free base(K201 free base)也是横纹肌中兰尼碱受体(ryanodine receptors)的部分激动剂。JTV-519 free base (K201 free base)是一种心脏保护剂,具有抗心律失常作用。 靶点 Calcium Channel   体外研究 JTV-519 (K201) inhibits inward Ca2+ movement into large unilamellar vesicles (LUV) caused by annexin V in a dosedependent manner.In the presence of 50nM annexin V and 400μM Ca2+,3μM JTV-519 shows significant inhibition of Ca2+ movement due to annexin V,and 50% inhibition is achieved at 25μM K201. 体内研究 JTV-519 (0.5mg/kg/h,i.v.,2h 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. Animal Model: Wild type male C57BL/6 mice weighing 18-22g with polymicrobial sepsis produced by cecal ligation and puncture (CLP). Dosage: 0.5mg/kg/h Administration: Applied intraperitoneally 2h before the surgery Result: Improved cardiac function,where the EF and FS were significantly increased.
保存条件:2-8℃