Home Cell Cycle ROCK inhibitor Ripasudil hydrochloride dihydrate For research use only.

Ripasudil hydrochloride dihydrate

Synonyms: K-115 hydrochloride dihydrate

Ripasudil hydrochloride dihydrate is a potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

Ripasudil hydrochloride dihydrate Chemical Structure

Ripasudil hydrochloride dihydrate Chemical Structure

CAS: 887375-67-9

Selleck's Ripasudil hydrochloride dihydrate has been cited by 8 publications

Purity & Quality Control

Batch: S799501 Water] 79 mg/mL] false] DMSO] 26 mg/mL] false] Ethanol] 5 mg/mL] false Purity: 99.22%
99.22

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Biological Activity

Description Ripasudil hydrochloride dihydrate is a potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
Targets
ROCK2 [1]
(Cell-free assay)		 ROCK1 [1]
(Cell-free assay)
19 nM 51 nM
In vitro
In vitro

In monkey trabecular meshwork (TM) cells, Ripasudil induces retraction and rounding of cell bodies as well as disruption of actin bundles. In Schlemm's canal endothelial (SCE) cells, Ripasudil significantly decreases transendothelial electrical resistance (TEER), increases the transendothelial flux of FITC-dextran, and disrupts cellular localization of ZO-1 expression. [3]
Kinase Assay Kinase Inhibition Assay
ROCK 1 (0.75 ng/μL) and ROCK 2 (0.5 ng/μL) are incubated with various concentrations of K-115, Y-27632, or HA-1077 at 25 °C for 90 min in 50 mmol/L Tris-HCl buffer (pH 7.5) containing 100 mmol/L KCl, 10 mmol/L MgCl2, 0.1 mmol/L EGTA, 30 μmol/L Long S6 Kinase Substrate peptide, and 1 μmol/L ATP in a total volume of 40 μL. PKACα, PKC, and CaMKIIα are also incubated with various concentrations of K-115, Y-27632, or HA-1077. PKACα (0.0625 ng/μL) is incubated at 25 °C for 30 min in 40 mmol/L Tris-HCl buffer (pH 7.5) containing 20 mmol/L MgCl2, 1 mg/mL BSA, 5 μmol/L Kemptide peptide substrate, and 1 μmol/L ATP in a total volume of 40 μL. PKC (0.025 ng/μL) is incubated at 25 °C for 80 min in 20 mmol/L Tris-HCl buffer (pH 7.5) containing 20 mmol/L MgCl2, 0.4 mmol/L CaCl2, 0.1 mg/mL BSA, 0.25 mmol/L EGTA, 25 ng/mL phosphatidylserine, 2.5 ng/mL diacylglycerol, 0.0075% Triton-X-100, 25 μmol/L DTT, 10 μmol/L Neurogranin (28–43) peptide substrate, and 1 μmol/L ATP in a total volume of 40 μL. CaMKIIα (0.025 ng/μL) is incubated at 25 °C for 90 min in 50 mmol/L Tris-HCl buffer (pH 7.5) containing 10 mmol/L MgCl2, 2 mmol/L CaCl2, 0.04 mg/mL BSA, 16 μg/mL purified calmodulin from bovine testis, 500 μmol/L DTT, 50 μmol/L Autocamitide 2, and 1 μmol/L ATP in a total volume of 40 μL. After incubation, 40 μL of Kinase-Glo 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.
In Vivo
In vivo

In albino rabbits and monkeys, topical instillation of Ripasudil significantly reduces intraocular pressure (IOP) with maximum IOP reduction of 8.55 mmHg and 4.36 mmHg at 0.5 % and 0.4%, respectively. [1]

Ripasudil (1 mg/kg daily, p.o.) exerts a neuroprotective effect on retinal ganglion cell (RGC) after optic nerve crush (NC) by suppressing oxidative stress through pathways involving the Nox family in a mouse model. [2]
Animal Research Animal Models Male C57BL/6 mice
Dosages 1 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04621136 Completed Retinopathy of Prematurity Kyushu University November 1 2020 Phase 1|Phase 2

Chemical lnformation & Solubility

Molecular Weight 395.88 Formula

C15H18FN3O2S.Cl H.2 H2 O
CAS No. 887375-67-9 SDF Download Ripasudil hydrochloride dihydrate SDF
Smiles CC1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)F.O.O.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 79 mg/mL

DMSO : 26 mg/mL ( (65.67 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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