223645-67-8
223645-67-8 结构式
基本信息
化合物BAY 41-2272
Ripasudil
k115 free base
K-115, Ripasudil
RIPASUDIL HYDROCHLOIDE
RIPASUDIL FREE BASE
K 115 FREE BASE
K115 FREE BASE
4-Fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline
Isoquinoline, 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]-
物理化学性质
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 5mg | 1600元 |
| 2024/04/30 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 10 mM * 1 mLin DMSO | 1760元 |
| 2024/04/30 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 10mg | 2600元 |
常见问题列表
|
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.