ROCK-IN-4 是一种有效的ROCK抑制剂，能够维持 NO 释放能力。ROCK-IN-4 可逆地解聚 F-肌动蛋白，并抑制人小梁网 (HTM) 细胞的线粒体呼吸。ROCK-IN-4 可用于青光眼或高眼压的研究。
| 生物活性 | ROCK-IN-4 is a potentROCKinhibitor 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]. |
体外研究
(In Vitro) | ROCK-IN-4 (RNO-6) (10 μM; 1 h) decreases p-MLC level and induces reversible F-actin depolymerization[1].
ROCK-IN-4 (10 μM; 24 h) involves in cGMP activation, increases cGMP concentration in human trabecular meshwork (HTM) cells[1].
ROCK-IN-4 (10 μM; 1 h) suppresses mitochondrial respiration by releasing NO and remarkably decreases the basal respiration, maximal respiration, and ATP production[1].
Western Blot Analysis[1] | Cell Line: | Human trabecular meshwork (HTM) cells | | Concentration: | 10 μM | | Incubation Time: | 1 hour | | Result: | Inhibited the phosphorylation of MLC, reduced the level of p-MLC. |
Immunofluorescence[1] | Cell Line: | Human trabecular meshwork (HTM) cells | | Concentration: | 10 μM | | Incubation Time: | 1 hour | | Result: | Exhibited conspicuous F-actin depolymerization, and after recovery for 4 h, recovered F-actin to the polymerization morphology, indicating a reversible depolymerization effect without permanent damage to cells. |
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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