YC-001 (C09-1185-543)

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 degenerationIn VitroYC-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 EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: NIH3T3 cells Concentration: 0.5, 1, 5, 10, 20, 40 µM Incubation Time: Result: Improved the glycosylation profile of P23H opsin.In VivoYC-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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-week-old Abca4 −/−Rdh8−/− mice Dosage: 50, 200mg/kg Administration: I.P. Result: Protected Abca4−/−Rdh8−/− mice from bright light-induced retinal degeneration. Animal Model: C57BL/6 mouse Dosage: 200 mg/kg Administration: I.P. Result: Entered mouse eyes after systemic administration but is not retained for prolonged periods. Animal Model: C57BL/6 mice Dosage: 100 mg/kg, 200 mg/kg Administration: I.p.; daily, 24 days Result: Showed no acute toxicity.Form:SolidIC50& Target:rod opsin. Specification: 0.99 Molecular Formula: C12H7ClO2S2 Molecular Weight: 282.77 PubChem CID: 2377702 Isomeric SMILES: C1C(=C(C(=O)O1)C2=CC=CS2)C3=CC=C(S3)Cl