RHO-激酶抑制剂
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) |
| InChI | InChI=1S/C14H17N3O3S.ClH/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17;/h1,3-5,7,15H,2,6,8-10H2,(H,16,18);1H |
| InChIKey | XWWFOUVDVJGNNG-UHFFFAOYSA-N |
| SMILES | c1c(S(=O)(=O)N2CCNCCC2)c2ccnc(O)c2cc1.Cl |
RHO-激酶抑制剂 用途与合成方法
|
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.
RHO-激酶抑制剂 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026-09-15 | HY-13911AR | RHO-激酶抑制剂 | 155558-32-0 | 5 mg | 1400 |
| 2026-09-15 | HY-13911AR | RHO-激酶抑制剂 | 155558-32-0 | 10 mg | 2100 |