14696-74-3 Purity
96%
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Specification
Rho-associated coiled-coil kinase (ROCK) inhibitors protect against neurodegeneration. This work determined the effects of the ROCK inhibitor Y-27632 on neuroprotection after kainate (KA)-induced seizures in mice and during glutamate-induced excitotoxicity in HT22 cells.
Evaluation Methods and Results
· Fluoro-Jade B staining and rapid Golgi staining demonstrated that Y-27632 provides protection against neurodegeneration and neurite dystrophy caused by KA.
· Western blot analysis indicated that Y-27632 reduced the levels of RhoA and ROCK2 in the hippocampus of KA-treated mice.
· Immunohistochemical analysis identified ROCK2-positive neurons and astrocytes in the hippocampus affected by KA.
· Furthermore, in HT22 cells, Y-27632 safeguarded neurons and supported neurite formation during in vitro glutamate-induced excitotoxicity.
· These findings suggested that inhibiting ROCK can influence neurite development and shield neurons from cell death due to excitotoxicity.
The aim of this work was to determine if the Rho-associated kinase (ROCK) inhibitor Y-27632 drops can be used to prevent severe corneal endothelial damage after surgical invasion. Result indicated that ROCK inhibitor Y-27632 could be made into eye drops to treat acute corneal endothelial injury to prevent bullous keratopathy.
· Formulation of Y-27632 eye drops
To make Y-27632 eye drops, Y-27632 (10 mM) was prepared by dissolving it in phosphate-buffered saline (PBS; 50 μL) and applying the solution to nine eyes in a corneal endothelial injury model four times daily. Meanwhile, PBS was given at the same frequency to nine control eyes.
· Evaluation methods and results
In the rabbit, Y-27632-treated eyes were observed more Ki67-positive cells than control eyes. Five of the six corneas exposed to Y-27632 had become transparent; none of the six control corneas did (P<0.01). Actin fibers were seen strongly at the cell cortex in Y-27632 eyes while control eyes had partial disruption of actin distribution along with the presence of stress fibers. Expression of N-cadherin and Na+/K+-ATPase was almost all-present in Y-27632 cells, but low in control cells. Preliminary human data showed that ROCK inhibitor eye drops had very promising results in corneal edema after cataract surgery.
The molecular formula of Rock inhibitor Y-27632 is C14H23Cl2N3O.
The synonyms of Rock inhibitor Y-27632 are Y-27632 dihydrochloride, 129830-38-2, Y-27632 2HCl, and Y 27632 dihydrochloride.
The molecular weight of Rock inhibitor Y-27632 is 320.3 g/mol.
The IUPAC name of Rock inhibitor Y-27632 is 4-[(1R)-1-aminoethyl]-N-pyridin-4-ylcyclohexane-1-carboxamide;dihydrochloride.
The InChI of Rock inhibitor Y-27632 is InChI=1S/C14H21N3O.2ClH/c1-10(15)11-2-4-12(5-3-11)14(18)17-13-6-8-16-9-7-13;;/h6-12H,2-5,15H2,1H3,(H,16,17,18);2*1H/t10-,11?,12?;;/m1../s1.
The InChIKey of Rock inhibitor Y-27632 is IDDDVXIUIXWAGJ-DDSAHXNVSA-N.
The other identifiers of Rock inhibitor Y-27632 include CAS number 129830-38-2, European Community (EC) number 813-428-5, UNII Q9828II7F3, DSSTox Substance ID DTXSID3042635, Wikidata ID Q27287129, and ChEMBL IDs CHEMBL536267 and CHEMBL1605605.
The hydrogen bond donor count of Rock inhibitor Y-27632 is 4.
The hydrogen bond acceptor count of Rock inhibitor Y-27632 is 3.
The topological polar surface area of Rock inhibitor Y-27632 is 68 Ų.