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TM5441

产品编号 T4254 CAS 1190221-43-2

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

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TM5441, CAS 1190221-43-2

规格	价格/CNY	货期
1 mg	￥ 362	现货
2 mg	￥ 518	现货
5 mg	￥ 815	现货
10 mg	￥ 1,230	现货
25 mg	￥ 2,660	现货
50 mg	￥ 3,930	现货
100 mg	￥ 5,730	现货
500 mg	￥ 11,800	现货
1 mL * 10 mM (in DMSO)	￥ 885	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor 1 (PAI-1).
靶点活性	Tumor cell lines:9.7～60.3 μM
体外活性	1.TM5441 inhibits branching of human umbilical vein endothelial cells (HUVECs) in a vasculature assay in vitro when used at a concentration of 50 μM but does not affect HUVEC survival or apoptosis. 2.TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC50 ranging between 9.7 and 60.3 μM. TM5441 decreases tumor cell viability in part through diminished proliferation. TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441is a potent stimulators of intrinsic apoptosis in tumor 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
体内活性	1.It also disrupts tumor vasculature in HT1080 and HCT116 mouse xenograft models when used at a dose of 20 mg/kg per day. TM5441 prevents hypertension and cardiac hypertrophy and reduces periaortic fibrosis induced by L-NAME . It protects against high-fat diet-induced non-alcoholic fatty liver disease (NAFLD) in mice when administered concurrently with a high-fat diet or after glucose tolerance has developed. TM5441 also increases median lifespan by 4-fold and reduces signs of senescence in Klotho-deficient mice, a mouse model of aging.2.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 effectively inhibits albuminuria, mesangial expansion, ECM accumulation, and macrophage infiltration in diabetic kidneys
激酶实验	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.
动物实验	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.

分子量	428.82
分子式	C21H17ClN2O6
CAS No.	1190221-43-2

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 300 mg/mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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):e201572012. 3. Boe AE,etal.Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence.Circulation. 2013 Nov 19;128(21):2318-24. 4. Lee SM,etal.TM5441, a plasminogen activator inhibitor-1 inhibitor, protects against high fat diet-induced non-alcoholic fatty liver disease.Oncotarget. 2017 Sep 21;8(52):89746-89760. 5. Eren M,etal.PAI-1-regulated extracellular proteolysis governs senescence and survival in Klotho mice.Proc Natl Acad Sci U S A. 2014 May 13;111(19):7090-5.

文献引用

1. Zhang W, Yang S, Chen D, et al. SOX2-OT induced by PAI-1 promotes triple-negative breast cancer cells metastasis by sponging miR-942-5p and activating PI3K/Akt signaling. Cellular and Molecular Life Sciences. 2022, 79(1): 1-16.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

TM5441 1190221-43-2 Apoptosis Metabolism PAI-1 Plasminogen activator inhibitor-1 Inhibitor TM 5441 TM-5441 inhibit inhibitor

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TM5441

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溶解度

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参考文献

文献引用

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剂量换算

体内实验配液计算器

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