2. Metabolic Enzyme/Protease
  3. RPE65
  4. 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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EYE-003

EYE-003 Chemical Structure

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EYE-003 Related Antibodies

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Description

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)[1].

In Vitro

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 Related Antibodies
In Vivo

EYE-003 (10 mg/kg, i.p., 30 min pre-photobleach, 2 h dark recovery) reduces 11-cis-retinal (11cRAL) synthesis and increases all-trans-retinyl esters (atREs) in BALB/cJ mice[1].
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.

Animal Model: BALB/cJ mice (6-8 weeks old, dark-adapted for 24 h)[1]
Dosage: 10 mg/kg
Administration: i.p., 30 min pre-photobleach, 2 h dark recovery
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.
Animal Model: BALB/cJ mice (6-8 weeks old, dark-adapted for 24 h)[1]
Dosage: 10 mg/kg
Administration: i.p., 0.5-4 h post-administration, 2 h dark recovery after photobleach
Result: Restored 11cRAL and atREs levels to vehicle group levels at 4 h post-administration in BALB/cJ mice.
Animal Model: Abca4⁻/⁻ Rdh8⁻/⁻ mice[1]
Dosage: 10 mg/kg
Administration: i.p. or i.g., 30 min pre-light exposure, single dose
Result: Reduced retinal autofluorescent puncta and homogeneous lipofuscin autofluorescence.
Preserved ONL thickness and maintains rod, S-cone, and M-cone ERG b-wave amplitudes.
Molecular Weight

339.43

Formula

C18H29NO5
SMILES

O=CO.CCCC(CCC)C(OC1=CC=CC(C(O)CCN)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EYE-003 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EYE-003EYE003EYE 003RPE65Retinal pigment epithelium 65 kDa proteinStargardt disease type 111-cis-retinalall-trans-retinyl estersInhibitorinhibitorinhibit

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