羥基法舒地爾
| 中文名稱 | 羥基法舒地爾 |
|---|---|
| 中文同義詞 | 法舒地爾雜質(zhì)L;5-[(六氫-1H-1,4-二氮雜卓-1-基)磺?；鵠-1(2H)-異喹啉酮;1 - [(1,2-二氫-1-氧代-5-異喹啉基)磺?；鵠六氫-1H-1,4-二氮雜鹽酸鹽;5-((1,4-二氮雜卓-1-基)磺?；?異喹啉-1(2H)-酮;5-((1,4-二氮雜環(huán)庚烷-1-基)磺酰基)異喹啉-1(2H)-酮;法舒地爾23;1-[(1,2-二氫-1-氧代-5-異喹啉YL)磺?；鵠六氫-1H-1,4-二氮雜卓;羥基法舒地爾,10 MM DMSO 溶液 |
| 英文名稱 | 1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE |
| 英文同義詞 | 5-(1,4-diazepane-1-sulfonyl)-1,2-dihydroisoquinolin-1-one;HYDROXYFASUDIL;HA-1100;HA 1100;HA1100;1-[(1,2-DIHYDRO-1-OXO-5-ISOQUINOLINYL)SULFONYL]HEXAHYDRO-1H-1,4-DIAZEPINE;1H-1,4-Diazepine, hexahydro-1-((1,2-dihydro-1-oxo-5-isoquinolinyl)sulfonyl)-;Ha 1100;Hexahydro-1-((1,2-dihydro-1-oxo-5-isoquinolinyl)sulfonyl)-1H-1,4-diazepine;1-[(1,2-Dihydro-1-oxo-5-isoquinolinyl)sulfonyl]hexahydro-1H-1,4-diazepinehydrochloride;HA 1100 HYDROCHLORIDE |
| CAS號(hào) | 105628-72-6 |
| 分子式 | C14H17N3O3S |
| 分子量 | 307.37 |
| EINECS號(hào) | |
| 相關(guān)類別 | 細(xì)胞周期;Angiogenesis and Metastasis;Intracellular signaling |
| Mol文件 | 105628-72-6.mol |
| 結(jié)構(gòu)式 |  |
羥基法舒地爾 性質(zhì)
| 儲(chǔ)存條件 | Sealed in dry,Store in freezer, under -20°C |
|---|---|
| 溶解度 | 溶于二甲基亞砜 |
| 形態(tài) | 固體 |
| 顏色 | 白色至米白色 |
| InChI | InChI=1S/C14H17N3O3S/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) |
| InChIKey | ZAVGJDAFCZAWSZ-UHFFFAOYSA-N |
| SMILES | C1(=O)C2=C(C(S(N3CCCNCC3)(=O)=O)=CC=C2)C=CN1 |
|
ROCK2 0.72 μM (IC 50 ) |
ROCK1 0.73 μM (IC 50 ) |
PKA 37 μM (IC 50 ) |
Hydroxyfasudil 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.
安全信息
| 毒性 | mouse,LD50,unreported,145mg/kg (145mg/kg),United States Patent Document. Vol. #4678783, |
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| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-13911 | 羥基法舒地爾 Hydroxyfasudil | 105628-72-6 | 1 mg | 155元 |
| 2026/06/05 | HY-13911 | 羥基法舒地爾 Hydroxyfasudil | 105628-72-6 | 5 mg | 390元 |