TM5441 is an orally bioavailable fibrinogen activator inhibitor-1 inhibitor that inhibits several cancer cell lines with IC50 values ranging from 13.9 to 51.1 μM.It induces intrinsic cell death in several human cancer cells and attenuates Nω-nitro-1-arginine methyl ester-induced cardiac hypertension and vascular senescence.

Tumor cell lines:9.7～60.3 μM

方法：使用TM5441（1-100μM）研究 HT1080、HCT116、Daoy、MDA-MB-231 和 Jurkat细胞的存活率。
结果：TM5441处理的细胞活力显着呈剂量依赖性降低50范围在 13.9 和 51.1μM之间.[2]
方法：人内皮细胞 EA.hy926 的培养物用 TM5441 （10 μM） 预处理 24 小时，然后多柔比星 （Dox） 处理一式三份，持续 4 天。从三个独立处理的孔中收集总蛋白和RNA并合并，探讨TM5441对Dox诱导的细胞衰老的保护作用。
结果：TM5441治疗可抑制Dox诱导的人内皮细胞中 p53、PAI-1、p16、p21 和 IGFBP3 的表达水平。[3]

方法：高脂饮食（HFD）喂养的C57BL/6J小鼠每天用20mg/kg的TM5441处理，研究TM5441（一种缺乏出血风险的口服 PAI-1 抑制剂）对HFD诱导的NAFLD的影响。
结果：TM5441早期和延迟治疗可减少肝脂肪变性，这两种策略都消除了肝脏胰岛素抵抗和线粒体功能障碍，表现为增强的 p-Akt 和 p-GSK3β、减少 p-JNK 信号传导以及 p-AMPK 和 PGC-1α激活。[1]

TM5441 is dissolved with DMSO at a stock concentration of 50 mM.HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells are treated with 0-100 μM TM5441 for 48 hours at 37°C. Cell viability is measured by MTT assay.

TM5441 is prepared in 0.5% carboxymethyl cellulose.Mice: TM5275 at 50 mg/kg/day and TM5441 at 10 mg/kg/day were orally administered in control and diabetic mice for 16 weeks. Mice were monitored at least once a day. At the end, blood is collected for measurement of plasma glucose and creatinine, urine for protein measurement, and kidneys for immunohistochemical analysis.