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。
货号:ajcx37508
CAS:748778-73-6
分子式:C12H7ClO2S2
分子量：282.77
溶解度:DMSO : 100 mg/mL (353.64 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

YC-001 is an inverse agonist and antagonist of rod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration[1].

YC-001 (0-100 µM) shows a potency activity of 8.7 µM and an efficacy at 150-310%[1].YC-001 (0.5, 1, 5, 10, 20, 40 µM) improves the glycosylation profile of P23H opsin mutant[1].YC-001 (0,-1.5 µM) reversibly binds rod opsin with EC50 OF 0.98 µM[1].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[1].

YC-001 (50, 200mg/kg; i.p.) protects Abca4-/-Rdh8-/- mice from bright light-induced retinal degeneration[1].YC-001 (200mg/kg; i.p.) enters mouse eyes after systemic administration but is not retained for prolonged periods[1].YC-001 (100 mg/kg, 200 mg/kg; i.p.; daily for 24 days) shows virtually no acute toxicity[1].

[1]. Chen Y, et al. A novel small molecule chaperone of rod opsin and its potential therapy for retinal degeneration. Nat Commun. 2018 May 17;9(1):1976.