| Identification | Back Directory | [Name]
1H-1,4-Diazepine-1-carboxylic acid, 4-[(4-fluoro-5-isoquinolinyl)sulfonyl]hexahydro-3-methyl-, 4-(nitrooxy)butyl ester, hydrochloride (1:1), (3S)- | [CAS]
2488395-07-7 | [Synonyms]
ROCK-IN-4
1H-1,4-Diazepine-1-carboxylic acid, 4-[(4-fluoro-5-isoquinolinyl)sulfonyl]hexahydro-3-methyl-, 4-(nitrooxy)butyl ester, hydrochloride (1:1), (3S)- | [Molecular Formula]
C20H26ClFN4O7S | [MOL File]
2488395-07-7.mol | [Molecular Weight]
520.96 |
| Hazard Information | Back Directory | [Uses]
ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. ROCK-IN-4 reversibly depolymerizes F-actin, and suppresses mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be used for glaucoma or ocular hypertension research[1]. | [in vivo]
ROCK-IN-4 (0.26% w/v for 10 μL; o.p. in right eye; single dose) exhibits significant IOP lowering and (0.26% w/v for 10 μL; o.p.; 10 d) exerts visual function and retinal ganglion cell (RGC) protection activities in glaucoma mouse model[1].
ROCK-IN-4 (0.579% w/v for 25 μL; o.p. in left eye; single dose) shows low hyperemic effect and eye irritation in New Zealand White rabbits[1].
| Animal Model: | Chronic Ocular Hypertension Mouse Model induced by Microbead[1] | | Dosage: | 0.26% (w/v), 10 μL | | Administration: | Ophthalmic drop; singel dose; administration in right eye 7 days after modeling, and measured IOP prior to and at 1, 2, 3, 4, and 6 h after instillation | | Result: | Reduced IOP (mmHg) to 3.68 ± 0.5 mmHg (19.9%) and 1.36 ± 0.6 mmHg (7.4%) at 1 and 4 h after instillation, respectively. |
| Animal Model: | New Zealand White rabbits[1] | | Dosage: | 0.579% (w/v); 25 μL | | Administration: | Ophthalmic drop; singel dose; administration in left eye before and at 1, 2, and 4 h after the first instillation | | Result: | Showed low side effects in conjunctival hyperemia. |
| [References]
[1] Yang Z, et al. Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities. J Med Chem. 2022 Aug 25. DOI:10.1021/acs.jmedchem.2c00600 |
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