K201 HEMIFUMARATE

生物活性体外研究体内研究 K201 HEMIFUMARATE 试剂级价格

K201 HEMIFUMARATE

CAS号:145903-06-6
英文名:K201 hemifumarate
中文名:K201 HEMIFUMARATE
CBNumber:CB92750672
分子式:C25H32N2O2S
分子量:424.6
MOL File:145903-06-6.mol

K201 HEMIFUMARATE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: soluble10mg/mL, clear
形态 :powder
酸度系数(pKa) :8.93±0.10(Predicted)
颜色 :white to beige
BRN :10598851

安全信息

危险品标志 :N,Xn
危险类别码 :50/53-53-22
安全说明 :60-61
危险品运输编号 :UN 3077 9 / PGIII
WGK Germany :3

K201 HEMIFUMARATE性质、用途与生产工艺

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.