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RPE65-61

Chemical Structure : RPE65-61

CAS No.: 2883452-77-3

RPE65-61 ((±)-RPE65-61)

Catalog No.: PC-20107Not For Human Use, Lab Use Only.

RPE65-61 ((±)-RPE65-61) is a selective, non-retinoid and uncompetitive inhibitor of RPE65 (a key enzyme in the visual cycle), inhibits the retinol isomerase activity of RPE65 in vitro with IC50 of 80 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    RPE65-61 ((±)-RPE65-61) is a selective, non-retinoid and uncompetitive inhibitor of RPE65 (a key enzyme in the visual cycle), inhibits the retinol isomerase activity of RPE65 in vitro with IC50 of 80 nM.
    (±)-RPE65-61 (375 nM) resulted in a significant decrease of 11-cis-retinol production in in vitro isomerase test using bovine RPE microsomes, did not suppress the production of retinyl ester implying that ecithin retinol acyltransferase (LRAT) was not inhibited.
    (±)-RPE65-61 also showed no activity in the Retinol-Binding Protein 4 (RBP4) binding assays.
    (±)-RPE65-61 (2 mg/kg, i.p.) delayed chromophore regeneration, reduced 11-cis-retinal and rhodopsin regeneration in the mouse eye in BALB/cJ mice, with higher levels of all-trans-retinyl ester, RPE65's substrate, indicating reduced RPE65 activity.
    (±)-RPE65-61 (2 mg/kg, i.p.) prevented declines of retinal thickness induced by light damage, preserved photoreceptors in light-induced retinal damage (LIRD) model.
    (±)-RPE65-61 down-regulated the cGAS-STING pathway, decreased the inflammatory factor, and attenuated retinal apoptosis caused by LIRD, which led to the preservation of the retinal function.

    Physicochemical Properties

    M.Wt 296.43
    Formula C15H24N2O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (2-aminoethyl)(3-(cyclohexylmethoxy)phenyl)(imino)-l6-sulfanone

    References

    1. Wang Y, et al. PLoS One. 2022 Oct 13;17(10):e0269437.

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