货号	规格	价格	上海	北京	珠海	重庆	武汉
S87620-2mg买3赠1	99.90%	￥80.00 S87620-2mg ￥80.00 现货（买3赠1）	9 9	-	-	-	-
S87620-5mg买3赠1	99.90%	￥100.00 S87620-5mg ￥100.00 现货（买3赠1）	6 6	-	-	-	-
S87620-10mg买3赠1	≥98%	￥180.00 S87620-10mg ￥180.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S87620-25mg买3赠1	≥98%	￥380.00 S87620-25mg ￥380.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S87620-100mg买3赠1	≥98%	￥1100.00 S87620-100mg ￥1100.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-

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产品描述：

TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence

靶点：

IC50: 13.9~51.1 μM (Tumor cell lines);PAI-1; Apoptosis

体外研究：

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

体内研究：

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

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.332 ml	11.66 ml	23.32 ml
5 mM	0.466 ml	2.332 ml	4.664 ml
10 mM	0.233 ml	1.166 ml	2.332 ml
50 mM	0.047 ml	0.233 ml	0.466 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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