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

EYE-003 是一种具有口服活性的 RPE65 抑制剂，IC50 值为 102 nM。EYE-003 通过减少 11-cis-Retinal (11cRAL) (HY-116711) 合成并增加全反式视黄酯 (atREs) 来调节小鼠的视觉循环。EYE-003 抑制暗视视网膜电图 (ERG) b-波振幅，并在 Abca4⁻/⁻ Rdh8⁻/⁻ 小鼠中通过以剂量依赖方式减少视网膜自发荧光斑点和保护外核层 (ONL) 厚度，发挥对视网膜变性的保护作用。EYE-003 可用于研究与视觉循环相关的视网膜病变，如斯塔加特病1型 (STGD1)。

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EYE-003

EYE-003 Chemical Structure

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EYE-003 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

EYE-003 (0.1-10 μM) 在牛视网膜色素上皮 (RPE) 微粒体中抑制 RPE65 活性，IC50 值为 102 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EYE-003 相关抗体:
体内研究
(In Vivo)

EYE-003 (10 mg/kg，腹腔注射，光漂白前 30 分钟给药，2 小时暗恢复) 减少 BALB/cJ 小鼠中 11-顺视黄醛 (11cRAL) 的合成，并增加全反式视黄酯 (atREs) [1]。
EYE-003 (10 mg/kg，腹腔注射，给药后 0.5-4 小时，光漂白后 2 小时暗恢复) 在给药后 4 小时将 BALB/cJ 小鼠的 11cRAL 和 atREs 水平恢复到对照组水平 [1]。
EYE-003 (10 mg/kg，口服灌胃，光漂白前 30 分钟给药，2 小时暗恢复) 显著抑制 BALB/cJ 小鼠的暗视视网膜电图 (ERG) a-波和 b-波振幅 [1]。
EYE-003 (10 mg/kg，腹腔注射或口服灌胃，光暴露前 30 分钟给药，单次剂量) 减少 Abca4⁻/⁻ Rdh8⁻/⁻ 小鼠的视网膜自发荧光斑点和均匀的脂褐素自发荧光，并保护外核层 (ONL) 厚度 [1]。

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.
分子量

339.43

Formula

C18H29NO5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

EYE-003 相关分类

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  • 稀释计算器

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  • 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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