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• 产品描述： Ripasudil (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51/19 nM for ROCK1/ROCK2).

• 靶点： ROCK

• 体外研究：
  Ripasudil shows less potent inhibitory activities against CaMKIIα, PKACα, and PKC (IC50s: 370 nM, 2.1 μM and 27 μM). Ripasudil (1, 10 μM) induces cytoskeletal changes, including retraction and cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. Ripasudil (5 μM) significantly reduces transendothelial electrical resistance (TEER) and increases FITC-dextran permeability in Schlemm's canal endothelial (SCE) cell monolayers

• 体内研究：
  Ripasudil reduces intraocular pressure 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 (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

• 细胞实验： Trabecular meshwork (TM) cells are plated on 6 well plates at a density of 1×10^4 cells per well in DMEM containing 10% FBS. Following overnight culture, when cells have reached semiconfluence, 1 or 10μM of Ripasudil, 10μM of Y-27632, or 10μM of fasudil are added to culture wells. PBS is used as a control vehicle. After 60min, drug solutions are removed and replaced with DMEM containing 10% FBS. Cells are observed by phase-contrast microscopy and photographed 60min after drug application and 2h after drug removal. For immunohistochemistry, TM cells are plated on gelatin-coated 8 well chamber slides at a density of 1×10^4 cells per well in DMEM containing 10% FBS. After overnight culture, when cells reach semiconfluence, cells are incubated in Ripasudil at 1 or 10μM, Y-27632 at 10μM, or fasudil at 10μM for 60min. PBS is used as a control vehicle. Drug solutions are removed and replaced with DMEM containing 10% FBS after 2h. Cells are fixed with 4% paraformaldehyde in PBS for 15min then washed with cytoskeletal

• 动物实验： In the rabbit experiments, 50 mL of vehicle or Ripasudil at concentrations of 0.0625%, 0.125%, 0.25, or 0.5% is instilled into one eye. Intraocular pressure (IOP) is measured in both eyes before and 0.5, 1, 2, 3, 4, and 5 h after instillation. The contralateral eye is not treated. Animals are administered all concentrations of Ripasudil assigned using the Latin square method with intervals of at least 2 d. In the monkey experiments, 20 mL of Ripasudil at concentrations of 0.1%, 0.2%, or 0.4%, and latanoprost at a concentration of 0.005% are instilled into one eye. IOP is measured in both eyes before and 1, 2, 4, 6, and 8 h after instillation. The contralateral eye is not treated. Animals are arranged to receive all formulations with intervals of at least 1 week using the Latin square method. The IOPs are compared with the results for the instillation side at pre-dose and at each time point after the instillation of Ripasudil and are compared with both eyes at each time point.

• 参考文献：
  1.Kaneko Y, et al. Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells. Sci Rep. 2016 Jan 19;6:19640. 2. Isobe T, et al. Effects of K-115, a rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr Eye Res. 2014 Aug;39(8):813-22. 3. Yamamoto K, et al. The novel Rho kinase (ROCK) inhibitor K-115: a new candidate drug for neuroprotective treatment in glaucoma. Invest Ophthalmol Vis Sci. 2014 Oct 2;55(11):7126-36.

• 溶解性： Soluble  in  H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.526 ml	12.63 ml	25.26 ml
  5 mM	0.505 ml	2.526 ml	5.052 ml
  10 mM	0.253 ml	1.263 ml	2.526 ml
  50 mM	0.051 ml	0.253 ml	0.505 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *