EYE-003
EYE-003 is an orally active RPE65 inhibitor with an IC50 of 102 nM. EYE-003 regulates the visual cycle in mice by reducing 11-cis-retinal (11cRAL) (HY-116711) synthesis and increasing all-trans-retinyl esters (atREs). EYE-003 suppresses scotopic ERG b-wave amplitude and exerts protective effects against retinal degeneration in Abca4⁻/⁻ Rdh8⁻/⁻ mice (a STGD1 model) by reducing retinal autofluorescent puncta and preserving outer nuclear layer (ONL) thickness in a dose-dependent manner. EYE-003 can be used for the study of visual cycle-associated retinopathies, such as Stargardt disease type 1 (STGD1).
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- Formule: C18H29NO5
- Masse moléculaire:339.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
EYE-003 (0.1-10 μM) inhibits RPE65 activity in bovine RPE microsomes with an IC50 of 102 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
EYE-003 (10 mg/kg, i.p., 0.5-4 h post-administration, 2 h dark recovery after photobleach) restores 11cRAL and atREs levels to vehicle group levels at 4 h post-administration in BALB/cJ mice[1].
EYE-003 (10 mg/kg, oral gavage, 30 min pre-photobleach, 2 h dark recovery) significantly suppresses both scotopic ERG a-wave and b-wave amplitudes in BALB/cJ mice[1].
EYE-003 (10 mg/kg, i.p. or i.g. , 30 min pre-light exposure, single dose) reduces retinal autofluorescent puncta and homogeneous lipofuscin autofluorescence, and preserves outer nuclear layer (ONL) thickness in Abca4⁻/⁻ Rdh8⁻/⁻ mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cJ mice (6-8 weeks old, dark-adapted for 24 h)[1]
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Dosage:10 mg/kg
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Administration:i.p., 30 min pre-photobleach, 2 h dark recovery
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Result:Reduced 11-cis-retinal (11cRAL) synthesis by 78%.
Increased all-trans-retinyl esters (atREs).
Recovered 80% of scotopic ERG a- and b-wave amplitudes at 8 h dark adaptation.
Reduced retinal autofluorescent puncta, preserves outer nuclear layer (ONL) thickness, and maintained scotopic ERG a- and b-wave amplitude.
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Animal Model:BALB/cJ mice (6-8 weeks old, dark-adapted for 24 h)[1]
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Dosage:10 mg/kg
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Administration:i.p., 0.5-4 h post-administration, 2 h dark recovery after photobleach
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Result:Restored 11cRAL and atREs levels to vehicle group levels at 4 h post-administration in BALB/cJ mice.
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Animal Model:Abca4⁻/⁻ Rdh8⁻/⁻ mice[1]
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Dosage:10 mg/kg
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Administration:i.p. or i.g., 30 min pre-light exposure, single dose
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Result:Reduced retinal autofluorescent puncta and homogeneous lipofuscin autofluorescence.
Preserved ONL thickness and maintains rod, S-cone, and M-cone ERG b-wave amplitudes.
Chemical Information
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Masse moléculaire 339.43
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Formule C18H29NO5
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SMILES
O=CO.CCCC(CCC)C(OC1=CC=CC(C(O)CCN)=C1)=O
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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)
EYE-003 Related Classifications
HY-175664 Related Classifications
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