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Ripasudil

产品编号 TQ0319 CAS 887375-67-9

别名: K-115, 瑞舒地尔盐酸二水合物, Ripasudil hydrochloride dihydrate

Ripasudil (Ripasudil hydrochloride dihydrate) 是一种 ROCK 特异性抑制剂，能够抑制 ROCK1和 ROCK2的活性，IC50值分别为 51 和 19 nM。

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Ripasudil, CAS 887375-67-9

规格	价格/CNY	货期
1 mg	￥ 547	现货
2 mg	￥ 783	现货
5 mg	￥ 1,330	现货
10 mg	￥ 2,160	现货
25 mg	￥ 3,690	现货
50 mg	￥ 5,330	现货
100 mg	￥ 7,520	现货
500 mg	￥ 14,800	现货
1 mL * 10 mM (in DMSO)	￥ 1,150	现货

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其他形式的 Ripasudil:

Ripasudil free base
询价

选择批次

纯度: 100%

纯度: 99.28%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Ripasudil (Ripasudil hydrochloride dihydrate) (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51/19 nM for ROCK1/ROCK2).
靶点活性	ROCK1:51 nM, ROCK2:19 nM, CaMK IIa:370 nM, PKC:27 μM, PKACa:2.1 μM
体外活性	Ripasudil 对CaMKIIα、PKACα和PKC的抑制活性较弱（IC50分别为370 nM、2.1 μM和27 μM）[1]。在培养的小梁细胞（TM细胞）中，Ripasudil（1、10 μM）可引起细胞骨架的变化，包括细胞收缩和圆化以及肌动蛋白束的减少。此外，Ripasudil（5 μM）显著降低Schlemm's管内皮（SCE）细胞单层的跨内皮电阻（TEER），并增加FITC-右旋糖酐的通透性[2]。
体内活性	Ripasudil在浓度依赖的方式下降低猴眼内0.1%至0.4%之间以及兔眼内0.0625%至0.5%之间的眼内压[1]。Ripasudil（1 mg/kg，p.o. 每日一次）在神经压迫(NC)后对视网膜神经节细胞(RGCs)表现出神经保护效果。此外，Ripasudil还能抑制小鼠轴突损伤引起的氧化应激。Ripasudil在NC损伤后抑制RGCs中依时间产生的ROS[3]。
激酶实验	ROCK 1 (0.75 ng/mL) and ROCK 2 (0.5 ng/mL) are incubated with various concentrations of Ripasudil, Y-27632, or HA-1077 at 25°C for 90 min in 50 mM Tris-HCl buffer (pH 7.5) containing 100 mM KCl, 10 mM MgCl2, 0.1 mM EGTA, 30 mM Long S6 Kinase Substrate peptide, and 1 mM ATP in a total volume of 40 mL. PKACa, PKC, and CaMKIIa are also incubated with various concentrations of Ripasudil, Y-27632, or HA-1077. PKACa (0.0625 ng/mL) is incubated at 25°C for 30 min in 40 mM Tris-HCl buffer (pH 7.5) containing 20 mM MgCl2, 1 mg/ mL BSA, 5 mM Kemptide peptide substrate, and 1 mM ATP in a total volume of 40 mL. PKC (0.025 ng/mL) is incubated at 25°C for 80 min in 20 mM Tris-HCl buffer (pH 7.5) containing 20 mM MgCl2, 0.4 mM CaCl2, 0.1 mg/mL BSA, 0.25 mM EGTA, 25 ng/mL phosphatidylserine, 2.5 ng/mL diacylglycerol, 0.0075% Triton-X-100, 25 mM DTT, 10 mM Neurogranin (28-43) peptide substrate, and 1 mM ATP in a total volume of 40 mL. CaMKIIa (0.025 ng/mL) is incubated at 25°C for 90 min in 50 mM Tris-HCl buffer (pH 7.5) containing 10 mM MgCl2, 2 mM CaCl2, 0.04 mg/mL BSA, 16 mg/mL purified calmodulin from bovine testis, 500 mM DTT, 50 mM Autocamitide 2, and 1 mM ATP in a total volume of 40 mL. After incubation, 40 mL of KinaseGlo Luminescent Kinase Assay solution is added, and allowed to remain at 25°C for 10 min, and Relative Light Units (RLU) are measured using a luminometer. The RLU without test compound is set as 100% (Control value), and that without enzyme and compound is set as 0% (Normal value). The reaction rate (% of control) is then calculated from the RLU with addition of each concentration of test compounds, and the 50% inhibitory concentrations (IC50) are determined by logistic regression analysis using SAS [1].
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 10?μM of Ripasudil, 10?μM of Y-27632, or 10?μM of fasudil are added to culture wells. PBS is used as a control vehicle. After 60?min, drug solutions are removed and replaced with DMEM containing 10% FBS. Cells are observed by phase-contrast microscopy and photographed 60?min after drug application and 2?h 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 10?μM, Y-27632 at 10?μM, or fasudil at 10?μM for 60?min. PBS is used as a control vehicle. Drug solutions are removed and replaced with DMEM containing 10% FBS after 2?h. Cells are fixed with 4% paraformaldehyde in PBS for 15?min then washed with cytoskeletal buffer (10?mM MES, 150?mM NaCl, 5?mM EGTA, 5?mM MgCl2, 5?mM glucose, pH 6.1) and serum buffer (10% FBS in PBS). Cells are permeabilized with 0.5% Triton X-100 in PBS for 12?min at room temperature and blocked with serum buffer for at least 2?h at 4°C. Filamentous actin (F-actin) is labeled with 0.05?mg/mL Phalloidin-TRITC for 1?h at room temperature. After washing with PBS, cells are mounted with a commercial mounting medium containing DAPI and observed using a fluorescence microscope. The exposure to take images for F-actin and DAPI are 0.1 and 0.05?sec, respectively [2].
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.

别名	K-115, 瑞舒地尔盐酸二水合物, Ripasudil hydrochloride dihydrate
分子量	395.88
分子式	C15H23ClFN3O4S
CAS No.	887375-67-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 45 mg/mL (113.67 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O	1 mM	2.526 mL	12.6301 mL	25.2602 mL	63.1504 mL
	5 mM	0.5052 mL	2.526 mL	5.052 mL	12.6301 mL
	10 mM	0.2526 mL	1.263 mL	2.526 mL	6.315 mL
	20 mM	0.1263 mL	0.6315 mL	1.263 mL	3.1575 mL
	50 mM	0.0505 mL	0.2526 mL	0.5052 mL	1.263 mL
	100 mM	0.0253 mL	0.1263 mL	0.2526 mL	0.6315 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. 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. 2. 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. 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.

文献引用

1. Sun L, Sun L, Li X, et al. A Novel Tigecycline Adjuvant ML-7 Reverses the Susceptibility of Tigecycline-Resistant Klebsiella pneumoniae. Frontiers in cellular and infection microbiology. 2022: 1341.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Ripasudil 887375-67-9 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK inhibit K-115 K115 Ripasudil Hydrochloride Rho-kinase Rho-associated kinase ROK 瑞舒地尔盐酸二水合物 Ripasudil hydrochloride Dihydrate Ripasudil hydrochloride dihydrate Inhibitor K 115 Rho-associated protein kinase inhibitor

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Ripasudil

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

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剂量换算

体内实验配液计算器

技术支持

Keywords