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Ripasudil

Catalog No. TQ0319 CAS 887375-67-9

Synonyms: K-115, Ripasudil hydrochloride dihydrate

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

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Ripasudil, CAS 887375-67-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 64.00
2 mg	In stock	$ 94.00
5 mg	In stock	$ 157.00
10 mg	In stock	$ 256.00
25 mg	In stock	$ 567.00
50 mg	In stock	$ 813.00
100 mg	In stock	$ 1,130.00
500 mg	In stock	$ 2,260.00
1 mL * 10 mM (in DMSO)	In stock	$ 173.00

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Purity: 100%

Purity: 99.28%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ripasudil (Ripasudil hydrochloride dihydrate) (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51/19 nM for ROCK1/ROCK2).
Targets&IC50	ROCK1:51 nM, ROCK2:19 nM, CaMK IIa:370 nM, PKC:27 μM, PKACa:2.1 μM
In vitro	Ripasudil shows less potent inhibitory activities against CaMKIIα, PKACα, and PKC (IC50s: 370 nM, 2.1 μM and 27 μM) [1]. 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 [2].
In vivo	Ripasudil effectively lowers intraocular pressure in a concentration-dependent manner, showing activity within the 0.1% to 0.4% range for monkey eyes and 0.0625% to 0.5% for rabbit eyes. Additionally, at a dosage of 1 mg/kg orally administered daily, it demonstrates a neuroprotective effect on retinal ganglion cells (RGCs) following nerve crush (NC). Furthermore, Ripasudil combats oxidative stress triggered by axonal injury in mice and inhibits the time-dependent increase of reactive oxygen species (ROS) production in RGCs after NC injury.
Kinase Assay	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].
Cell Research	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].
Animal Research	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.

Synonyms	K-115, Ripasudil hydrochloride dihydrate
Molecular Weight	395.88
Formula	C15H23ClFN3O4S
CAS No.	887375-67-9

Storage

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

Solubility Information

H2O: 45 mg/mL (113.67 mM)

References and Literature

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.

Citations

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library FDA-Approved Kinase Inhibitor Library Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Kinase Inhibitor Library TGF-beta/Smad Compound Library Neural Regeneration Compound Library Bioactive Compounds Library Max

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Thiazovivin Y-27632 ROCK-IN-2 YAP/TAZ inhibitor-1 Chroman 1 ROCK-IN-9 ROCK inhibitor-2 CCG-232964

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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 Ripasudil hydrochloride Dihydrate Ripasudil hydrochloride dihydrate Inhibitor K 115 Rho-associated protein kinase inhibitor

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