MY-5445

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Chemical Structure| 78351-75-4 同义名 : -
CAS号 : 78351-75-4
货号 : A304814
分子式 : C20H14ClN3
纯度 : 99%
分子量 : 331.8
MDL号 : MFCD00209838
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(150.69 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 MY-5445 acts as a specific antagonist of cyclic GMP phosphodiesterase, particularly PDE5, exhibiting a Ki value of 1.3 μM. It effectively prevents human platelet aggregation and modulates the ATP-binding cassette transporter ABCG2 selectively, leading to an anti-proliferative effect[1][2]. Additionally, MY-5445 curbs human platelet aggregation by elevating cyclic GMP levels, serving as a valuable tool for investigating the role of cyclic GMP in this process[1]. MY-5445 selectively counteracts the ABCG2-mediated multidrug resistance in cells with high levels of ABCG2. It enhances the effectiveness of an ABCG2 substrate drug against ABCG2-overexpressing cancer cells resistant to multiple drugs, likely through altering ABCG2's function and/or expression. Additionally, a 48-hour treatment with MY-5445 at a concentration of 3 μM significantly augments apoptosis in S1-M1-80 cells induced by topotecan[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.07mL

3.01mL

1.51mL

30.14mL

6.03mL

3.01mL
参考文献

[1]Souness JE, et al. Role of selective cyclic GMP phosphodiesterase inhibition in the myorelaxant actions of M&B 22,948, MY-5445, vinpocetine and 1-methyl-3-isobutyl-8-(methylamino)xanthine. Br J Pharmacol. 1989 Nov;98(3):725-34.

[2]Chung-Pu Wu, et al. MY-5445, a phosphodiesterase type 5 inhibitor, resensitizes ABCG2-overexpressing multidrug-resistant cancer cells to cytotoxic anticancer drugs. Am J Cancer Res. 2020; 10(1): 164-178.

[3]Maud Bollenbach, et al. Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model. Eur J Med Chem. 2019 Sep 1;177:269-290.