MY-5445 是特异性的 cGMP 磷酸二酯酶PDE5抑制剂,其Ki=1.3 μM。它是一种ABCG2转运蛋白调节剂,具有抗增殖活性。它能抑制人血小板凝集。
产品描述
MY-5445 is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM).
体外活性
in ABCG2-overexpressing cells, MY-5445 selectively reverses ABCG2-mediated multidrug resistance. 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]. In the S1-M1-80 cell, MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis[2].
体内活性
I.p administration of 0.5-3 mg/kg twice a day for 15 days) produces significant relief of mechanical hypersensitivity[3].
Cas No.
78351-75-4
分子式
C20H14ClN3
分子量
331.8
别名
N-(3-chlorophenyl)-4-phenylphthalazin-1-amine
储存和溶解度
DMSO:40 mg/mL (120.55 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years