1. Metabolic Enzyme/Protease
  2. RPE65
  3. EYE-002

EYE-002 是一种 RPE65 抑制剂,IC50 值为 69 nM。EYE-002 促进小鼠暗视视网膜电图 (ERG) a-/b-波振幅的恢复。EYE-002 通过减少 11-cisretinal (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-002 对小鼠光性视网膜损伤具有保护作用。EYE-002 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-002

EYE-002 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EYE-002 is a RPE65 inhibitor with an IC50 of 69 nM. EYE-002 promotes recovery of scotopic ERG a-/b-wave amplitudes. EYE-002 regulates the visual cycle in mice by reducing 11-cis-retinal (11cRAL) (HY-116711) synthesis and increasing all-trans-retinyl esters (atREs). EYE-002 exerts protective effects against photic retinal damage in mice. EYE-002 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-002 (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 69 nM[1]

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

体内研究
(In Vivo)

EYE-002 (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-002 (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 11 cRAL 和 atREs 水平恢复到对照组水平[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.
分子量

311.37

Formula

C16H25NO5

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
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  • 稀释计算器

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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.

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产品名称:
EYE-002
目录号:
HY-175663
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