RPE65-61 | RPE65 inhibitor | Probechem Biochemicals

Chemical Structure : RPE65-61

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RPE65-61 ((±)-RPE65-61)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	296.43
分子式	C15H24N2O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2-aminoethyl)(3-(cyclohexylmethoxy)phenyl)(imino)-l6-sulfanone

参考文献

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

RPE65-61 ((±)-RPE65-61)

生物&药学活性

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RPE65-61 ((±)-RPE65-61)

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物理化学性质&存储条件

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