Information Ripasudil (K-115) hydrochloride dihydrate is potentROCKinhibitor withIC50of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension. Targets ROCK2 (Cell-free assay); ROCK1 (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. 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.
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
Ripasudil (K-115) hydrochloride dihydrate
CAS number：887375-67-9 molecular formula：C15H18FN3O2S.ClH.2H2O
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 1H-1,4-Diazepine, 1-((4-fluoro-5-isoquinolinyl)sulfonyl)hexahydro-2-methyl-, monohydrochloride, dihydrate, (2S)- | 4-Fluoro-5-[(2S)-2-methyl-1,4-diazepane-1-sulfonyl]isoquinoline dihydrate hydrochloride | Ripasudil HCl dihydrate | Ripasudil hydrochloride | ||
| CAS number | 887375-67-9 | molecular formula | C15H18FN3O2S.ClH.2H2O |
| molecular weight | 395.88 g/mol | Exact mass | ≥99% |
| PSA | 72.700 Ų | logp | 0.739 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
