PDE5 1.3 μM (Ki) PDE5 6.7 μM (IC 50 ) PDE4 37 μM (IC 50 )

MY-5445 (0.5-3 mg/kg; i.p.; twice a day; for 15 days) produces a significant relief of mechanical hypersensitivity. Animal Model: C57BL/6J male mice Dosage: 0.5 mg/kg, 3 mg/kg Administration: Intraperitoneal injection, twice a day, for 15 days Result: Alleviated the cuff-induced allodynia.

MY-5445 inhibits human platelet aggregation by increasing cyclic GMP content and that it provides a useful probe for elucidating the role of cyclic GMP in platelet aggregation . MY-5445 selectively reverses ABCG2-mediated multidrug resistance in ABCG2-overexpressing cells. MY-5445 reverses ABCG2-mediated multidrug resistance (MDR) by potentiating the cytotoxicity of an ABCG2 substrate drug in ABCG2-overexpressing multidrug-resistant cancer cells, possibly by modulating the function and/or the protein expression of ABCG2. MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis in S1-M1-80 cell. Apoptosis Analysis Cell Line: Human S1 colon cancer cells, S1-M1-80 cancer cells Concentration: 3 μM Incubation Time: 48 hours Result: Enhanced drug-induced apoptosis in ABCG2-overexpressing cancer cells.

MY-5445 是一种特异性的 cGMP 磷酸二酯酶 PDE5 抑制剂，其 Ki 值为 1.3 μM。MY-5445 能抑制人血小板凝集。MY-5445 是一种 ABCG2 转运蛋白调节剂，具有抗增殖活性。