| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H26ClFN4O7S |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
ROCK-IN-4 is a potent ROCK inhibitor that retains nitric oxide (NO)-releasing ability. It reversibly depolymerizes F-actin and suppresses mitochondrial respiration in human trabecular meshwork (HTM) cells, and it can be used in glaucoma and ocular hypertension research[1]. Its molecular formula is C20H26ClFN4O7S, with a molecular weight of 520.96 g/mol.
Physical & Chemical Properties
| CAS Number | 2488395-07-7 |
|---|---|
| Molecular Formula | C20H26ClFN4O7S |
| Molecular Weight | 520.96 g/mol |
| SMILES | C[C@H]1CN(C(OCCCCO[N+]([O-])=O)=O)CCCN1S(=O)(C2=CC=CC3=C2C(F)=CN=C3)=O.[H]Cl |
| Signaling Pathway | Cell Cycle/DNA Damage; TGF-beta/Smad; Stem Cell/Wnt; Cytoskeleton |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
At 10 μM for 1 h, ROCK-IN-4 (RNO-6) lowers p-MLC levels and induces reversible F-actin depolymerization[1]. At 10 μM for 24 h, it takes part in cGMP activation and raises cGMP concentration in human trabecular meshwork (HTM) cells[1]. At 10 μM for 1 h, it also suppresses mitochondrial respiration by releasing NO and markedly lowers 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. |
In Vivo
In a glaucoma mouse model, a single o.p. dose of ROCK-IN-4 in the right eye (0.26% w/v for 10 μL) significantly lowers IOP, and o.p. dosing for 10 d (0.26% w/v for 10 μL) shows visual function and retinal ganglion cell (RGC) protection activities[1]. In New Zealand White rabbits, a single o.p. dose in the left eye (0.579% w/v for 25 μL) causes low hyperemic effect and eye irritation[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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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