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编 号：F753277
分子式：C20H26ClFN4O7S
分子量：520.96
分子式：C20H26ClFN4O7S
分子量：520.96
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CAS No: 2488395-07-7
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生物活性：
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.
体内研究：
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. 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.Animal Model:Chronic Ocular Hypertension Mouse Model induced by Microbead
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
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.
体外研究：
ROCK-IN-4 (RNO-6) (10 μM; 1 h) decreases p-MLC level and induces reversible F-actin depolymerization.ROCK-IN-4 (10 μM; 24 h) involves in cGMP activation, increases cGMP concentration in human trabecular meshwork (HTM) cells.ROCK-IN-4 (10 μM; 1 h) suppresses mitochondrial respiration by releasing NO and remarkably decreases the basal respiration, maximal respiration, and ATP production.
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.
体内研究：
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. 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.Animal Model:Chronic Ocular Hypertension Mouse Model induced by Microbead
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
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.
体外研究：
ROCK-IN-4 (RNO-6) (10 μM; 1 h) decreases p-MLC level and induces reversible F-actin depolymerization.ROCK-IN-4 (10 μM; 24 h) involves in cGMP activation, increases cGMP concentration in human trabecular meshwork (HTM) cells.ROCK-IN-4 (10 μM; 1 h) suppresses mitochondrial respiration by releasing NO and remarkably decreases the basal respiration, maximal respiration, and ATP production.
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