RHO-激酶抑制剂
| 中文名称 | RHO-激酶抑制剂 |
|---|---|
| 中文同义词 | 羟基法舒地尔盐酸盐;羟基法舒地尔;RHO-激酶抑制剂;1-(1-羟基-5-异喹啉磺酰基)高哌嗪盐酸盐;1-羟基法舒地尔;羟基法舒地尔单盐酸盐;5-[(1,4-二氮杂环庚烷-1-基)磺酰基]异喹啉-1(2H)-酮盐酸盐;法舒地尔杂质7(HCL) |
| 英文名称 | HYDROXYFASUDIL MONOHYDROCHLORIDE |
| 英文同义词 | 5-[(Hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-1(2H)-isoquinolinone;Hydroxyfasudil Hydrochloride;1-(1-hydroxy-5-isoquinolinesulfonyl)homopiperazine monohydrochloride;HYDROXYFASUDIL MONOHYDROCHLORIDE;Hydroxyfasudil hydrochloride hydrate,1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate;1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate;Hydroxyfasudil hydrochloride hydrate;Hydroxyfasudil (HA-1100) |
| CAS号 | 155558-32-0 |
| 分子式 | C14H18ClN3O3S |
| 分子量 | 343.82902 |
| EINECS号 | |
| 相关类别 | 杂质;Various Metabolites and Impurities;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals |
| Mol文件 | 155558-32-0.mol |
| 结构式 |  |
RHO-激酶抑制剂 性质
| 熔点 | >250 (dec.) |
|---|---|
| 储存条件 | Inert atmosphere,2-8°C |
| 溶解度 | 在水中的溶解度>5mg/mL |
| 形态 | 固体 |
| 颜色 | 白色 |
| 水溶解性 | Soluble in water (20mM) |
| InChIKey | XWWFOUVDVJGNNG-UHFFFAOYSA-N |
|
ROCK2 0.72 μM (IC 50 ) |
ROCK1 0.73 μM (IC 50 ) |
PKA 37 μM (IC 50 ) |
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.
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.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-13911A | Hydroxyfasudil hydrochloride | 1 mg | 280元 | |
| 2024/01/25 | HY-13911A | RHO-激酶抑制剂 Hydroxyfasudil hydrochloride | 155558-32-0 | 5mg | 700元 |