ROCK-IN-4
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.
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- CAS No.: 2488395-07-7
- Formule: C20H26ClFN4O7S
- Masse moléculaire:520.96
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human trabecular meshwork (HTM) cells
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Concentration:10 μM
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Incubation Time:1 hour
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Result:Inhibited the phosphorylation of MLC, reduced the level of p-MLC.
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Cell Line:Human trabecular meshwork (HTM) cells
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Concentration:10 μM
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Incubation Time:1 hour
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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.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chronic Ocular Hypertension Mouse Model induced by Microbead[1]
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Dosage:0.26% (w/v), 10 μL
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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
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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.
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Animal Model:New Zealand White rabbits[1]
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Dosage:0.579% (w/v); 25 μL
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Administration:Ophthalmic drop; singel dose; administration in left eye before and at 1, 2, and 4 h after the first instillation
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Result:Showed low side effects in conjunctival hyperemia.
Chemical Information
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CAS No. 2488395-07-7
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Masse moléculaire 520.96
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Formule C20H26ClFN4O7S
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SMILES
C[C@H]1CN(C(OCCCCO[N+]([O-])=O)=O)CCCN1S(=O)(C2=CC=CC3=C2C(F)=CN=C3)=O.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ROCK-IN-4 Related Classifications
HY-151189 Related Classifications
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