product name Ripasudil (K-115)
Description: Ripasudil (also known as K-115) is potent and selective ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, it is used for the treatment of glaucoma and ocular hypertension. Ripasudil, K-115, is a potent ROCK inhibitor. It is approved for use in Japan as a 0.4% ophthalmic solution. In rabbits, topical instillation of K-115 significantly reduced IOP in a dose-dependent manner.
References: Curr Eye Res. 2014 Aug;39(8):813-22; Sci Rep. 2016 Jan 19;6:19640.
395.88
Formula
C15H18FN3O2S. HCl. 2 H2O
CAS No.
887375-67-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 26 mg/mL warmed (65.7 mM)
Water: 79 mg/mL (199.5 mM)
Ethanol: 5 mg/mL (12.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In monkey trabecular meshwork (TM) cells, Ripasudil induces retraction and rounding of cell bodies as well as disruption of actin bundles. In Schlemms 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. Kinase Assay: Cell Assay: |
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| 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. 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Curr Eye Res. 2014 Aug;39(8):813-22; Sci Rep. 2016 Jan 19;6:19640. |
