K201 HEMIFUMARATE
| 中文名称 | K201 HEMIFUMARATE |
|---|---|
| 中文同义词 | 化合物 T11731;化合物 JTV-519 FREE BASE;145903-06-6;JTV-519 hemifumarate;【进口原装】JTV-519 hemifumarate/145903-06-6;【进口原装】JTV-519 hemifumarate/145903-06-6 |
| 英文名称 | K201 hemifumarate |
| 英文同义词 | 1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone hemifumarate;JTV-519 hemifumarate;K201 hemifumarate;1-(2,3-Dihydro-7-methoxy-1,4-benzothiazepin-4(5H)-yl)-3-[4-(phenylmethyl)-1-piperidinyl]-1-propanone;4-[3-(4-Benzylpiperidin-1-yl)propionyl]-7-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine;3-(4-benzylpiperidin-1-yl)-1-(7-methoxy-2,3-dihydrobenzo[f][1,4]thiazepin-4(5H)-yl)propan-1-one(K201 hemifumarate);JTV-519 (K201;JTV-519 free base |
| CAS号 | 145903-06-6 |
| 分子式 | C25H32N2O2S |
| 分子量 | 424.6 |
| EINECS号 | |
| 相关类别 | 标准品 |
| Mol文件 | 145903-06-6.mol |
| 结构式 |  |
K201 HEMIFUMARATE 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 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 8.93±0.10(Predicted) |
| 颜色 | 白色至米色 |
| BRN | 10598851 |
| InChIKey | MNAIJOCDPCXVEY-WXXKFALUSA-N |
| SMILES | OC(=O)\C=C\C(O)=O.COc1ccc2SCCN(Cc2c1)C(=O)CCN3CCC(CC3)Cc4ccccc4.COc5ccc6SCCN(Cc6c5)C(=O)CCN7CCC(CC7)Cc8ccccc8 |
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。
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.
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. |
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 |
| 存储类别 | 11 - 可燃固体 |
| 危险性类别 | 危害水生环境-急性危害 类别1 危害水生环境-长期危害 类别1 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-15293B | JTV-519 hemifumarate | 145903-06-6 | 5 mg | 750元 |
| 2025/12/22 | HY-15293B | K201 HEMIFUMARATE JTV-519 hemifumarate | 145903-06-6 | 10 mM * 1 mLin DMSO | 796元 |