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  3. ROCK-IN-4

ROCK-IN-4 

Cat. No.: HY-151189
Handling Instructions

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.

For research use only. We do not sell to patients.

ROCK-IN-4 Chemical Structure

ROCK-IN-4 Chemical Structure

CAS No. : 2488395-07-7

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Description

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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

520.96

Formula

C20H26ClFN4O7S

CAS No.
SMILES

C[[email protected]]1CN(C(OCCCCO[N+]([O-])=O)=O)CCCN1S(=O)(C2=CC=CC3=C2C(F)=CN=C3)=O.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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ROCK-IN-4
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HY-151189
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