A PAI-1 inhibitor; decreases survival of HT1080

TM5441 – 1 mg

Brand:
Cayman
CAS:
1190221-43-2
Storage:
-20
UN-No:
Non-Hazardous - /

TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor 1 (PAI-1), a serine-protease inhibitor involved in thrombosis.{37397,37395} It decreases survival of HT1080, HCT116, Daoy, MDA-MB-231, and Jurkat cancer cells with IC50 values ranging from 13.9 to 51.1 µM.{37397} 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. 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 (Item No. 80210).{37395} 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.{37398} TM5441 also increases median lifespan by 4-fold and reduces signs of senescence in Klotho-deficient mice, a mouse model of aging.{37396}  

 

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SKU: 22965 - 1 mg Category:

Description

A PAI-1 inhibitor; decreases survival of HT1080, HCT116, Daoy, MDA-MB-231, and Jurkat cancer cells (IC50s = 13.9-51.1 µM); inhibits branching of HUVECs (50 µM); disrupts tumor vasculature in mouse xenograft models (20 mg/kg per day); prevents L-NAME-induced hypertension and cardiac hypertrophy; protects against NAFLD in mice induced by high-fat diet

Formal name: 5-chloro-2-[[2-[2-[[3-(3-furanyl)phenyl]amino]-2-oxoethoxy]acetyl]amino]-benzoic acid

Synonyms: 

Molecular weight: 428.8

CAS: 1190221-43-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Blood Coagulation Factors||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cardiovascular System|Blood|Acute Phase Reactants||Research Area|Cardiovascular System|Blood|Thrombosis||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH

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