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TM5441

CAS No. : 1190221-43-2

MCE 站：TM5441

产品活性：TM5441 是一种口服生物可利用的纤溶酶原激活物抑制剂-1 抑制剂 (PAI-1)，抑制多个癌症细胞系的IC₅₀ 值在 13.9 到 51.1 μM，并诱导几种人类癌症细胞的内在调亡。TM5441 减弱 Nω-硝基-1-精氨酸甲酯诱导的心脏高血压和血管衰老。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：PAI-1  |  Apoptosis

In Vitro: TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC₅₀ ranging between 13.9 and 51.1 μM.
TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441 increases apoptosis in HT1080 and HCT116 cells.
TM5441 induces mitochondrial depolarization.
In mouse proximal tubular epithelial cells, TM5441 effectively inhibits PAI-1-induced mRNA expression of fibrosis and inflammation markers and also reverses PAI-1-induced inhibition of plasmin activity.

In Vivo: Oral administration of TM5441 (20 mg/kg daily) to HT1080 and HCT116 xenotransplanted mice increases tumor cell apoptosis and has a significant disruptive effect on the tumor vasculature that is associated with a decrease in tumor growth and an increase in survival. The average peak plasma concentration is 11.4 μM one hour after oral administration and undetectable levels 23 hours after administration.
TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence, prolongs lifespan in klotho null mice and elicits anti-tumorigenic and anti-angiogenic activities in cancer.

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