HYDROXYFASUDIL MONOHYDROCHLORIDE,英文名:HYDROXYFASUDIL MONOHYDROCHLORIDE,CAS:155558-32-0,化学式:C14H18ClN3
155558-32-0
HYDROXYFASUDIL MONOHYDROCHLORIDE(HYDROXYFASUDIL MONOHYDROCHLORIDE)
CAS: 155558-32-0
化学式: C14H18ClN3O3S
| 中文名 | HYDROXYFASUDIL MONOHYDROCHLORIDE |
| 英文名 | HYDROXYFASUDIL MONOHYDROCHLORIDE |
| 别名 | 羟基法舒地尔 1-羟基法舒地尔 羟基法舒地尔盐酸盐 RHO-激酶抑制剂 羟基法舒地尔单盐酸盐 1-(1-羟基-5-异喹啉磺酰基)高哌嗪盐酸盐 5-[(1,4-二氮杂环庚烷-1-基)磺酰基]异喹啉-1(2H)-酮盐酸盐 |
| 英文别名 | Hydroxyfasudil HCl HA1100 HYDROCHLORIDE HA-1100 HYDROCHLORIDE HA 1100 HYDROCHLORIDE Hydroxyfasudil Hydrochloride HYDROXYFASUDIL MONOHYDROCHLORIDE 5-(1,4-diazepan-1-ylsulfonyl)-2h-isoquinolin-1-one Hydroxyfasudil hydrochloride (HA-1100 hydrochloride) 5-[(Hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-1(2H)-isoquinolinone 1-(1-hydroxy-5-isoquinolinesulfonyl)homopiperazine monohydrochloride |
| CAS | 155558-32-0 |
| 化学式 | C14H18ClN3O3S |
| 分子量 | 343.82902 |
| InChIKey | XWWFOUVDVJGNNG-UHFFFAOYSA-N |
| 熔点 | >250 (dec.) |
| 溶解度 | H2O: >5 mg/mL |
| 存储条件 | Inert atmosphere,2-8°C |
| 外观 | 固体 |
| 颜色 | white |
| 体外研究 | Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC 50 s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC 50 of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC 50 value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM. |
| 体内研究 | Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SD rats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure. Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs). Furthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly ameliorates decreased penile cGMP contents in rats. |
| 危险品标志 | Xn - 有害物品 |
| 风险术语 | 22 - 吞食有害。 |
| WGK Germany | 3 |
155558-32-0 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.908 ml | 14.542 ml | 29.084 ml |
| 5 mM | 0.582 ml | 2.908 ml | 5.817 ml |
| 10 mM | 0.291 ml | 1.454 ml | 2.908 ml |
| 5 mM | 0.058 ml | 0.291 ml | 0.582 ml |
155558-32-0 - 简介
HYDROXYFASUDIL MONOHYDROCHLORIDE（羟基法舒地尔单盐酸盐）是一种化合物，它是法舒地尔的一个新的代谢产物。性质：
HYDROXYFASUDIL MONOHYDROCHLORIDE是一种白色或类白色结晶粉末，可溶于水和有机溶剂。
HYDROXYFASUDIL MONOHYDROCHLORIDE主要用于治疗缺血性脑血管病变和其他心血管疾病。它通过抑制Rho激酶的活性来扩张血管，改善血流。临床上常用于治疗脑血管痉挛引起的脑梗死和脑血管畸形等疾病。
HYDROXYFASUDIL MONOHYDROCHLORIDE可以通过法舒地尔与二甲基亚砜（DMSO）反应得到。反应中需要加热溶剂和触媒，得到的产物可经过结晶纯化得到最终的单盐酸盐结晶体。
安全信息：使用HYDROXYFASUDIL MONOHYDROCHLORIDE时需遵循相关安全操作规范。它的毒性和副作用有限，但仍然需要在医生的指导下使用。导致过敏反应的可能性较低，但个体差异存在。另外，对于患有严重肝功能和肾功能受损的患者，使用时需要谨慎。
最后更新：2024-04-10 22:30:50
