Ripasudil hydrochloride dihydrate | B2984

Ripasudil (K-115) is a potent inhibitor of Rho kinase (ROCK), with IC₅₀ values of 19 and 51 nM for ROCK-2 and ROCK-1, respectively. Ripasudil (10 μM) induces cytoskeletal changes, including retraction, cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. It significantly reduces transendothelial electrical resistance (TEER) and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers at a concentration of 5 μM. A 0.4% ophthalmic solution significantly lowers intraocular pressure (IOP) in rabbits and monkeys. It was the first ophthalmic solution developed for the treatment of glaucoma and ocular hypertension in Japan.

Ripasudil (K-115) is a potent inhibitor of Rho kinase (ROCK), with IC₅₀ values of 19 and 51 nM for ROCK-2 and ROCK-1, respectively. Ripasudil (10 μM) induces cytoskeletal changes, including retraction, cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. It significantly reduces transendothelial electrical resistance (TEER) and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers at a concentration of 5 μM. A 0.4% ophthalmic solution significantly lowers intraocular pressure (IOP) in rabbits and monkeys. It was the first ophthalmic solution developed for the treatment of glaucoma and ocular hypertension in Japan.

B2984 | Ripasudil hydrochloride dihydrate DataSheet

Alternate Name/Synonyms: 4-fluoro-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline, dihydrate, hydrochloride; K-115 Hydrochloride Dihydrate; 1H-1,4-Diazepine, 1-((4-fluoro-5-isoquinolinyl)sulfonyl)hexahydro-2-methyl-, monohydrochloride, dihydrate

Appearance: White powder

Formulation:

CAS Number: 887375-67-9

Structure Available?: True

Peptide sequence:

Salt Form: True

Molecular Formula: C₁₅H₂₃ClFN₃O₄S

Molecular Weight: 395.88

Cell-Permeable?: True

Purity: 0.99

Solubilities: 50 mg/ml in Water

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A potent Rho kinase (ROCK) inhibitor

MDL Number: MFCD26960897

PubChem CID: 11625386

SMILES: CC1CNCCCN1S(=O)(=O)C2=CC=CC3=CN=CC(=C32)F.O.O.Cl

InChi: InChI=1S/C15H18FN3O2S.ClH.2H2O/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14;;;/h2,4-5,9-11,17H,3,6-8H2,1H3;1H;2*1H2/t11-;;;/m0.../s1

InChi Key: CMDJNMACGABCKQ-XVSRHIFFSA-N