Ripasudil (K-115) hydrochloride dihydrate

Catalog No.S7995

For research use only.

Ripasudil (K-115) hydrochloride dihydrate is 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 (K-115) hydrochloride dihydrate Chemical Structure

CAS No. 887375-67-9

Selleck's Ripasudil (K-115) hydrochloride dihydrate has been cited by 4 Publications

Purity & Quality Control

Choose Selective ROCK Inhibitors

Other ROCK Products

Biological Activity

Description Ripasudil (K-115) hydrochloride dihydrate is 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 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]

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]

Protocol (from reference)

Animal Research:

[2]

  • Animal Models: Male C57BL/6 mice
  • Dosages: 1 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Water 79 mg/mL
(199.55 mM)
DMSO 26 mg/mL warmed
(65.67 mM)
Ethanol 5 mg/mL warmed
(12.63 mM)

Chemical Information

Molecular Weight 395.88
Formula

C15H18FN3O2S.Cl H.2 H2 O

CAS No. 887375-67-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)F.O.O.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04621136 Recruiting Drug: Ripasudil ophthalmic solution 0.4% Retinopathy of Prematurity Kyushu University November 1 2020 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ripasudil (K-115) hydrochloride dihydrate | Ripasudil (K-115) hydrochloride dihydrate supplier | purchase Ripasudil (K-115) hydrochloride dihydrate | Ripasudil (K-115) hydrochloride dihydrate cost | Ripasudil (K-115) hydrochloride dihydrate manufacturer | order Ripasudil (K-115) hydrochloride dihydrate | Ripasudil (K-115) hydrochloride dihydrate distributor