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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C18H29NO5
- 分子量:339.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
体内実験
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.
化学情報
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分子量 339.43
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分子式 C18H29NO5
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SMILES
O=CO.CCCC(CCC)C(OC1=CC=CC(C(O)CCN)=C1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)