MY-5445

MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a K_i of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect^[1][2]. IC50 & Target: PDE5^[1] In Vitro: 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 ^[1].
MY-5445 selectively reverses ABCG2-mediated multidrug resistance in ABCG2-overexpressing cells^[2].
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^[2].
MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis in S1-M1-80 cell^[2].
In Vivo: MY-5445 (0.5-3 mg/kg; i.p.; twice a day; for 15 days) produces a significant relief of mechanical hypersensitivity^[3].