RHO-激酶抑制劑
| 中文名稱 | RHO-激酶抑制劑 |
|---|---|
| 中文同義詞 | 羥基法舒地爾鹽酸鹽;羥基法舒地爾;RHO-激酶抑制劑;1-(1-羥基-5-異喹啉磺?；?高哌嗪鹽酸鹽;1-羥基法舒地爾;羥基法舒地爾單鹽酸鹽;5-[(1,4-二氮雜環(huán)庚烷-1-基)磺?；鵠異喹啉-1(2H)-酮鹽酸鹽;法舒地爾雜質(zhì)7(HCL) |
| 英文名稱 | HYDROXYFASUDIL MONOHYDROCHLORIDE |
| 英文同義詞 | 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 (HA-1100);HA-1100 HYDROCHLORIDE;HA 1100 HYDROCHLORIDE;HA1100 HYDROCHLORIDE |
| CAS號 | 155558-32-0 |
| 分子式 | C14H18ClN3O3S |
| 分子量 | 343.82902 |
| EINECS號 | |
| 相關(guān)類別 | 雜質(zhì);Various Metabolites and Impurities;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals |
| Mol文件 | 155558-32-0.mol |
| 結(jié)構(gòu)式 |  |
RHO-激酶抑制劑 性質(zhì)
| 熔點 | >250 (dec.) |
|---|---|
| 儲存條件 | Inert atmosphere,2-8°C |
| 溶解度 | 在水中的溶解度>5mg/mL |
| 形態(tài) | 固體 |
| 顏色 | 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 |
|
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 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-13911AR | RHO-激酶抑制劑 Hydroxyfasudil hydrochloride (Standard) | 155558-32-0 | 5 mg | 1400元 |
| 2026/06/05 | HY-13911AR | RHO-激酶抑制劑 Hydroxyfasudil hydrochloride (Standard) | 155558-32-0 | 10 mg | 2100元 |