Ripasudil (K-115) hydrochloride dihydrate

Catalog No.S7995

Ripasudil (K-115) hydrochloride dihydrate Chemical Structure

Molecular Weight(MW): 395.88

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.

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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

Animal Research:

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+ Expand
  • Animal Models: Male C57BL/6 mice
  • Formulation: --
  • Dosages: 1 mg/kg
  • Administration: p.o.
    (Only for Reference)

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)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 395.88
Formula

C15H18FN3O2S.Cl H.2 H2 O

CAS No. 887375-67-9
Storage powder
Synonyms N/A

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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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ROCK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID