145903-06-6
145903-06-6 结构式
基本信息
英文别名
JTV-519
(K201K201 free base
JTV-519 free base
K201 hemifumarate
JTV-519 hemifumarate
4-[3-(4-Benzylpiperidin-1-yl)propionyl]-7-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine
1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone
1-Propanone, 1-(2,3-dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-
1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone hemifumarate
3-(4-benzylpiperidin-1-yl)-1-(7-methoxy-2,3-dihydrobenzo[f][1,4]thiazepin-4(5H)-yl)propan-1-one(K201 hemifumarate)
物理化学性质
沸点615.1±55.0 °C(Predicted)
密度1.153±0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度DMSO：可溶10mg/mL，澄清
酸度系数(pKa)8.93±0.10(Predicted)
形态粉末
颜色白色至米色
BRN10598851
常见问题列表
生物活性
JTV-519 free base (K201 free base) 是 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。体外研究
JTV-519 (K201) inhibits inward Ca 2+ 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 Ca 2+ , 3 μM JTV-519 shows significant inhibition of Ca 2+ movement due to annexin V, and 50% inhibition is achieved at 25 μM K201.
体内研究
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.
| 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. |