RX-021
RX-021 is a ROCK1 and ROCK2 inhibitor with IC50 values of 30.01 nM and 34.31 nM, respectively. RX-021 induces reversible morphological changes in human trabecular meshwork cells, maintains the survival of retinal ganglion cells, restores electroretinogram responses, and improves retinal histopathological changes. RX-021 achieves sustained reduction of intraocular pressure in a mouse model of ocular hypertension. RX-021 can be used for the research of glaucoma.
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- Formule: C19H22N4
- Masse moléculaire:306.40
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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
Description
IC50 & Target
[1]|
ROCK1 30.01 nM (IC50) |
ROCK2 34.31 nM (IC50) |
In Vitro
RX-021 (20 μM) shows no cytotoxicity in HTM cells, maintaining a cell viability rate of 99.10% at the concentration of 20 μM[1].
RX-021 (1 μM; 2-24 h) induces reversible contraction of HTM cells at a concentration of 1 μM, with significant contraction observable at 4 h, and cell morphology almost fully recovers within 2 h after removal of the compound[1].
RX-021 (1 μM; 24-48 h) completely inhibits HTM cell-mediated collagen gel contraction for up to 48 h[1].
RX-021 (1 μM; 10-24 h) effectively inhibits TGF-β2-induced migration of HTM cells and reduces the wound closure rate at 10 h and 24 h[1].
RX-021 (1 μM; 1 h) reduces the overall oxygen consumption rate of HTM cells, but does not significantly alter key mitochondrial respiratory parameters, including basal respiration, ATP-coupled respiration, maximal respiratory capacity, spare respiratory capacity, or proton leak[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:10 h, 24 h
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Result:Attenuated TGF-β2-induced HTM cell migration at 10 h.
Attenuated TGF-β2-induced HTM cell migration at 24 h.
Reduced wound closure rates of TGF-β2-treated HTM cells at 10 h and 24 h post-treatment.
In Vivo
RX-021 (441 μM/5 μL; eye drop; once daily for 28 consecutive days) reduces IOP in a mouse model of long-term microsphere-induced ocular hypertension, with a slightly slower onset but a longer duration of action[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:441 μM/5 μL/eye
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Administration:eye drop; single dose
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Result:Decreased by 5.38 mmHg at 4 hours.
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Animal Model:male C57BL/6
mice (18-20 g)[1] -
Dosage:441 μM/5 μL/eye
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Administration:eye drop; once daily for 28 consecutive days
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Result:Brought the IOP back to normal starting from D21 and maintained it until D28.
Chemical Information
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Masse moléculaire 306.40
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Formule C19H22N4
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SMILES
CN(CC1)CCC1C2=CC=C(NC3=CC=NC4=C3C=CN4)C=C2
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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)
RX-021 Related Classifications
HY-187203 Related Classifications
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