MY-5445

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MY-5445 是 5 型磷酸二酯酶 (PDE5) 的特异性抑制剂。 MY-5445 选择性抑制 cGMP PDE (Ki:1.3 μM)。

MY-5445 is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM).(In Vitro): 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. In the S1-M1-80 cell, MY-5445 (3 μM; 48 hours) substantially increases the topotecan-induced apoptosis.(In Vivo):I.p administration of 0.5-3 mg/kg twice a day for 15 days) produces significant relief of mechanical hypersensitivity.

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 (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 daysResult:Alleviated the cuff-induced allodynia.

N-(3-chlorophenyl)-4-phenylphthalazin-1-amine

Angiogenesis

PDE

DHFR

——

——

78351-75-4

331.8

C20H14ClN3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (150.69 mM)

Clc1cccc(Nc2nnc(-c3ccccc3)c3ccccc23)c1

——

(-20℃)

With Ice Pack

≥ 2 years