RX-044
RX-044 is a ROCK1/ROCK2 inhibitor with ROCK1 IC50 10.01 nM and ROCK2 IC50 9.68 nM, and demonstrates kinase selectivity. RX-044 induces reversible cell retraction, modulates cytoskeletal organization via F-actin depolymerization, inhibits cell contractility, and attenuates TGF-β2-induced cell migration. RX-044 preserves retinal ganglion cell survival, restores electroretinography responses, and ameliorates histopathological changes. RX-044 lowers intraocular pressure in a mouse ocular hypertension model. RX-044 shows no cytotoxicity in target cells. RX-044 exhibits initial ocular irritation that subsides with extended dosing. RX-044 can be used for the research of glaucoma.
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- Fòrmula: C20H24N4
- Peso molecular:320.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
ROCK1 10.01 nM (IC50) |
ROCK2 9.68 nM (IC50) |
In Vitro
RX-044 (compound 39) potently and selectively inhibits purified ROCK1 and ROCK2 enzymes, with IC50 values of 10.01 nM and 9.68 nM, respectively, while exhibiting limited off-target activity against other kinases[1].
RX-044 (20 μM) shows no cytotoxicity in HTM cells, with cell viability maintained at 92.55%[1].
RX-044 (1 μM; 0-24 h) induces rapid, reversible retraction of HTM cells and regulates cytoskeletal structure via F-actin depolymerization[1].
RX-044 (1 μM; 24-48 h) inhibits HTM cell-mediated collagen gel contraction for at least 48 h, indicating a persistent inhibitory effect on cell contractility[1].
RX-044 (1 μM; 0-24 h) inhibits TGF-β2-induced migration of HTM cells[1].
RX-044 (1 μM; 1 h) modulates mitochondrial respiration in HTM cells, reducing basal respiration, ATP-coupled respiration and maximal respiratory capacity, without affecting spare respiratory capacity or proton leakage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HTM (human trabecular meshwork) cells
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Concentration:1 μM (co-treated with 10 ng/mL TGF-β2)
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Incubation Time:0, 10, 24 h
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Result:Attenuated TGF-β2-induced HTM cell migration.
Reduced wound closure rates after 24 h of co-treatment.
In Vivo
RX-044 (441 μM; topical eye drop administration once daily for 28 consecutive days) gradually restores elevated intraocular pressure in mice to normal levels starting from day 21 of administration; only mild conjunctival and iris hyperemia occurs at the initial stage of administration, and the irritant symptoms resolve completely after long-term continuous administration; meanwhile, it fully preserves the layered structure of the retina, increases the number of retinal ganglion cells labeled by BRN3A, restores the amplitudes of all characteristic waves in electroretinography, and ameliorates atrophic and inflammatory pathological damages of the cornea, iris and retina[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice with magnetic bead-induced ocular hypertension[1]
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Dosage:441 μM
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Administration:Topical ocular single administration; measured at 1, 2, 4, 6, 8, 24 h
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Result:Exhibited prominent intraocular pressure-lowering activity, and reached the maximal IOP drop of 3.66 mmHg at 4 h with sustained weak hypotensive effect within 24 h.
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Animal Model:Male C57BL/6 mice with polystyrene microsphere-induced ocular hypertension[1]
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Dosage:441 μM
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Administration:Topical ocular administration; once daily; for 28 days
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Result:Restored elevated IOP to normal levels from day 21 and maintained stable long-term efficacy, and induced no abnormal body weight fluctuations in mice.
Triggered mild conjunctival hyperemia, iris congestion and anterior chamber flare on day 7, and eliminated all ocular irritation symptoms after sustained administration.
Protected complete layered retinal structure and avoided retinal edema, detachment and hemorrhage on OCT scans.
Elevated the count of BRN3A-positive retinal ganglion cells and thickened retinal INL/ONL layers to reverse retinal atrophy lesions.
Recovered amplitudes of all core ERG wavesl.
Alleviated corneal hyperplasia, iris vasodilation, inflammatory infiltration and retinal structural disorganization validated by eyeball H&E staining.
- Scratch/Wound-Healing Migration Assay
- Mammalian live/dead viability and cytotoxicity staining
- Cell migration
- Neural Crest/Neuronal Cell Migration Explant Assay
- Research Protocol for Cardiovascular Diseases
- Phalloidin F-actin cytoskeleton staining
- Cell Viability Determination by MTT Colorimetric Assay
- Cell Cytotoxicity Assay
- Chemotaxis Gradient Chamber Assay 1
- Under-Agarose Cell Migration Assay
- Transwell/Boyden Chamber Migration Assay
- 3D Collagen/Hydrogel Matrix Migration Assay
- Cell-Exclusion Zone Migration Assay
- Chemotaxis Gradient Chamber Assay 2
Chemical Information
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Peso molecular 320.43
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Fòrmula C20H24N4
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SMILES
CN(CC1)CCC1C2=CC=C(NC3=CC=NC4=C3C(C)=CN4)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RX-044 Related Classifications
HY-187204 Related Classifications
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