Ripasudil
| 中文名称 | Ripasudil |
|---|---|
| 中文同义词 | 瑞舒地尔;化合物BAY 41-2272;(S)-4-氟-5-((2-甲基-1,4-二氮杂卓-1-基)磺酰基)异喹啉 |
| 英文名称 | Ripasudil |
| 英文同义词 | k115 free base;Ripasudil;4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline;RIPASUDIL FREE BASE;K 115 FREE BASE;K115 FREE BASE;CS-1564;K-115, Ripasudil;Isoquinoline, 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-;RIPASUDIL HYDROCHLOIDE |
| CAS号 | 223645-67-8 |
| 分子式 | C15H18FN3O2S |
| 分子量 | 323.39 |
| EINECS号 | |
| 相关类别 | 原料药;对照品 |
| Mol文件 | 223645-67-8.mol |
| 结构式 |  |
Ripasudil 性质
| 沸点 | 497.2±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.293±0.06 g/cm3(Predicted) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 9.70±0.40(Predicted) |
|
ROCK2 19 nM (IC 50 ) |
ROCK1 51 nM (IC 50 ) |
CaMKIIa 370 nM (IC 50 ) |
PKACa 2.1 μM (IC 50 ) |
PKC 27 μM (IC 50 ) |
Ripasudil (K-115) is a potent inhibitor of ROCK, with IC 50 s of 19 and 51 nM for ROCK2 and ROCK1, respectively. Ripasudil also shows less potent inhibitory activities against CaMKIIα, PKACα and PKC, with IC 50 s of 370 nM, 2.1 μM and 27 μM, respectively. Ripasudil (K-115; 1, 10 μM) induces cytoskeletal changes, including retraction and cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. Ripasudil (5 μM) sifnificantly reduces transendothelial electrical resistance (TEER), and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers.
Ripasudil (K-115) reduces intraocular pressure (IOP) in a concentration-dependent manner at concentrations between 0.1% and 0.4% in monkey eyes and 0.0625% to 0.5% in rabbit eyes, respectively. Ripasudil (K-115; 1 mg/kg, p.o. daily) shows a neuroprotective effect on retinal ganglion cells (RGCs) after nerve crush (NC). Ripasudil also inhibits the oxidative stress induced by axonal injury in mice. Ripasudil suppresses the time-dependent production of ROS in RGCs after NC injury.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 2mg | 1060元 |
| 2024/01/25 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 10 mM * 1 mLin DMSO | 1393元 |