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TM5441

Catalog No. T4254   CAS 1190221-43-2

TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor 1 (PAI-1).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
TM5441 Chemical Structure
TM5441, CAS 1190221-43-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 79.00
10 mg In stock $ 122.00
25 mg In stock $ 263.00
50 mg In stock $ 493.00
100 mg In stock $ 701.00
500 mg In stock $ 1,460.00
1 mL * 10 mM (in DMSO) In stock $ 88.00
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Purity: 99.09%
Purity: 98.87%
Purity: 98.87%
Purity: 98.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor 1 (PAI-1).
Targets&IC50 Tumor cell lines:9.7~60.3 μM
In vitro 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
In vivo 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
Kinase Assay 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.
Animal Research 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.
Molecular Weight 428.82
Formula C21H17ClN2O6
CAS No. 1190221-43-2

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 300 mg/mL

TargetMolReferences and Literature

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.

TargetMolCitations

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library NO PAINS Compound Library Apoptosis Compound Library Anti-Cancer Compound Library Inhibitor Library Target-Focused Phenotypic Screening Library Orally Active Compound Library Metabolism Compound Library Bioactive Compound Library Anti-Metabolism Disease Compound Library

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Keywords

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

 

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