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CAS No. : 748778-73-6
MCE 国际站:YC-001
产品活性:YC-001 是杆状视蛋白 (rod opsin) 的反向激动剂和拮抗剂。YC-001 可逆地结合视杆视蛋白并稳定视杆视蛋白的结构。YC-001 保护小鼠免受强光诱导的视网膜变性。YC-001 具有研究视网膜变性的潜力。
研究领域:Metabolic Enzyme/Protease
作用靶点:Endogenous Metabolite
In Vitro: YC-001 (0-100 µM) shows a potency activity of 8.7 µM and an efficacy at 150–310%.
YC-001 (0.5, 1, 5, 10, 20, 40 µM) improves the glycosylation profile of P23H opsin mutant.
YC-001 (0,-1.5 µM) reversibly binds rod opsin with EC50 OF 0.98 µM.
YC-001 (0.313, 0.625, 1.25, 2.5, 5, 10, 20, 80 µM) increases in cAMP level in a dose-dependent manner in NIH3T3 cells.
In Vivo: YC-001 (50, 200mg/kg; i.p.) protects Abca4−/−Rdh8−/− mice from bright light-induced retinal degeneration.
YC-001 (200mg/kg; i.p.) enters mouse eyes after systemic administration but is not retained for prolonged periods.
YC-001 (100 mg/kg, 200 mg/kg; i.p.; daily for 24 days) shows virtually no acute toxicity.
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