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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- 화학식: C18H29NO5
- 분자량:339.43
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
In Vitro
In Vivo
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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분자량 339.43
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화학식 C18H29NO5
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SMILES
O=CO.CCCC(CCC)C(OC1=CC=CC(C(O)CCN)=C1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)