Molecular Formula | C15H23ClFN3O4S |
Molar Mass | 395.8772232 |
Solubility | 10 mM in DMSO |
Storage Condition | -20℃ |
In vitro study | In monkey trabecular meshwork (TM) cells, Ripasudil induces contraction and encircling of the cell body, as well as disruption of actin bundles. In Schlem's duct endothelial (SCE) cells, Ripasudil significantly reduces transendothelial resistance (TEER), increases or decreases the transmembrane flux of FITC-dextran, and interferes with the cellular localization of ZO-1 expression. |
In vivo study | Topical instillation of Ripasudil significantly reduced intraocular pressure (IOP) in white rabbits and monkeys, with maximal IOP decreasing by 8.55 mmHg and 4.36 mmHg at 0.5 and 0.4 concentrations, respectively. In a mouse model, Ripasudil (1 mg/kg daily, p.o.) neuroprotective effects on retinal ganglion cells (RGC) following optic nerve injury (NC) by inhibiting oxidative stress in a pathway involving the Nox family. |
Risk Codes | R24/25 - R26 - Very Toxic by inhalation R28 - Very Toxic if swallowed |
Safety Description | S28 - After contact with skin, wash immediately with plenty of soap-suds. S38 - In case of insufficient ventilation, wear suitable respiratory equipment. S41 - In case of fire and / or explosion do not breathe fumes. S48 - To be kept wet with (there follows a material name). |
HS Code | 29339900 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.526 ml | 12.63 ml | 25.26 ml |
5 mM | 0.505 ml | 2.526 ml | 5.052 ml |
10 mM | 0.253 ml | 1.263 ml | 2.526 ml |
5 mM | 0.051 ml | 0.253 ml | 0.505 ml |
biological activity | Ripasudil (K-115) hydrochloride dihydrate is a potent ROCK Inhibitor, the IC50 for ROCK1 and ROCK2 were 51 nM and 19 nM, respectively, and were used for the treatment of glaucoma and intraocular hypertension. |
Target | Value |
ROCK2 (Cell-free assay) | 19 nM |
ROCK1 (Cell-free assay) | 51 nM |