TM5441

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Chemical Structure| 1190221-43-2 同义名 : -
CAS号 : 1190221-43-2
货号 : A843529
分子式 : C21H17ClN2O6
纯度 : 99%+
分子量 : 428.822
MDL号 : MFCD31382187
存储条件：

Pure form Inert atmosphere,Room Temperature

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

DMSO: 105 mg/mL(244.86 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
动物实验配方：
生物活性
描述 TM5441 is an orally bioavailable PAI-1 inhibitor with an IC50 ranging from 13.9 to 51.1 μM, capable of inducing intrinsic apoptosis in various human cancer cell lines. TM5441 can alleviate cardiac hypertension and vascular senescence induced by Nω-nitro-l-arginine methyl ester[1][2]. TM5441 inhibits the proliferation of HT1080, HCT116, Daoy, MDA-MB-231, and Jurkat cells in a dose-dependent manner, with IC50 values ranging from 13.9 to 51.1 μM. It also dose-dependently increases caspase 3/7 activity in HT1080 and HCT116 cells. Furthermore, TM5441 enhances apoptosis in these cells and induces mitochondrial depolarization[1]. In mouse proximal tubular epithelial cells, TM5441 effectively inhibits the fibrosis and inflammatory marker mRNA expression induced by PAI-1, and reverses the inhibition of plasminogen activator activity induced by PAI-1[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.32mL

4.66mL

2.33mL
参考文献

[1]Placencio VR, et al. Small Molecule Inhibitors of Plasminogen Activator Inhibitor-1 Elicit Anti-Tumorigenic and Anti-Angiogenic Activity. PLoS One. 2015 Jul 24;10(7):e0133786.

[2]Jeong BY, et al. Novel Plasminogen Activator Inhibitor-1 Inhibitors Prevent Diabetic Kidney Injury in a Mouse Model. PLoS One. 2016 Jun 3;11(6):e0157012.