223645-67-8
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
| 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 | Soluble in DMSO |
| 酸度系数(pKa) | 9.70±0.40(Predicted) |
| 形态 | powder |
| 颜色 | white to beige |
| 水溶解性 | H2O: 2mg/mL, clear |
| InChI | 1S/C15H18FN3O2S/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14/h2,4-5,9-11,17H,3,6-8H2,1H3/t11-/m0/s1 |
| InChIKey | QSKQVZWVLOIIEV-NSHDSACASA-N |
| SMILES | Fc1c2c(cnc1)cccc2[S](=O)(=O)N3[C@H](CNCCC3)C |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
| WGK Germany | WGK 3 |
| 存储类别 | 11 - Combustible Solids |
Ripasudil价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/12/22 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 2mg | 1060元 |
| 2025/12/22 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 5mg | 1600元 |
| 2025/12/22 | HY-15685 | Ripasudil Ripasudil | 223645-67-8 | 10 mM * 1 mLin DMSO | 1760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.